Search Result
Results for "
profile
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-P9989
-
|
REGN5458
|
CD3
TNF Receptor
|
Cancer
|
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Linvoseltamab is a bispecific antibody targeting to both BCMA (TNFRSF17) and CD3 epsilon. Linvoseltamab shows safety profile and encouraging efficacy in relapsed/refractory multiple myeloma (RRMM) models .
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-
-
- HY-W052051
-
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N-Acetylbenzylamine
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Endogenous Metabolite
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Others
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N-Benzylacetamide (N-Acetylbenzylamine), as an endogenous metabolite, is the major component of the plasma metabolic profile of Benznidazole (HY-B1548) .
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-
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- HY-133018
-
|
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HCV
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Infection
|
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HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity .
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-
-
- HY-133018A
-
|
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HCV
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Cancer
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HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity .
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-
-
- HY-155652
-
|
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BCRP
|
Cancer
|
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ABCG2-IN-1 (compound K2), a Ko143 analog, is an orally active ABCG2 inhibitor with an IC50 of 0.13 μM. ABCG2-IN-1 has favorable oral pharmacokinetic profiles in mice .
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-
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- HY-116183
-
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HCV
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Infection
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ITX 4520 is an orally active and potent hepatitis C virus inhibitor exhibiting an excellent PK profile in both rats and dogs .
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-
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- HY-115494
-
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Neladenoson bialanate hydrochloride; BAY-1067197 hydrochloride
|
Adenosine Receptor
|
Cardiovascular Disease
|
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Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) hydrochloride is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate hydrochloride has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
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-
-
- HY-123353
-
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Neladenoson bialanate; BAY-1067197
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Adenosine Receptor
|
Cardiovascular Disease
|
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Neladenoson dalanate (Neladenoson bialanate; BAY-1067197) is a orally active agonist precursor of partial Adenosine A1 Receptor. Neladenoson dalanate has a good pharmacokinetic and safety profile, can be used for the chronic heart diseases .
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-
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- HY-146380
-
|
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Histone Demethylase
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Cancer
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S1427 is a tranylcypromine-derived LSD1 inhibitor with the IC50 of 390 nM and Ki of 80 nM. S1427 exhibits desirable hERG channel inhibition and microsomal stability profiles. Inhibition of LSD1 partially reduces the proliferation of cancer cells .
|
-
-
- HY-10096
-
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GSK-3
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Neurological Disease
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TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
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-
-
- HY-103112A
-
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5-HT Receptor
|
Neurological Disease
|
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SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
|
-
-
- HY-103112B
-
|
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5-HT Receptor
|
Neurological Disease
|
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SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
|
-
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- HY-103112
-
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5-HT Receptor
|
Neurological Disease
|
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SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
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- HY-W075766
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Nickel difluoride
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Biochemical Assay Reagents
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Others
|
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Nickel(II) fluoride (Nickel difluoride) is a fluorinating agent and catalyst suitable for surface treatment of aluminum profiles and the production of inks, fluorescent lamps, and organic synthesis. Nickel(II) fluoride is a kind of biological materials or organic compounds that are widely used in life science research .
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- HY-10861
-
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5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile .
|
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- HY-148254
-
|
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Deubiquitinase
|
Cancer
|
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8RK64 is a covalent UCHL1 inhibitor (IC50: 0.32 μM) . 8RK64 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-115721
-
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Parasite
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Infection
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Antimalarial agent 2 is a novel orally efficacious antimalarials that suggests a fast in vitro killing profile.
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- HY-132867
-
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Pim
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Cancer
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MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.
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- HY-N2842
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Others
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Inflammation/Immunology
|
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α-Amyrin acetate, a natural triterpenoid, has anti-inflammatory activity, antispasmodic profile and the relaxant effect .
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- HY-W005178
-
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Endogenous Metabolite
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Others
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Octadecanedioic acid, an endogenous metabolite, is a long-chain dicarboxylic acid that has been found in serum free fatty acid profile in Reye syndrome .
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- HY-W011215
-
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Apoptosis
Reactive Oxygen Species
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Inflammation/Immunology
|
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Dihexyl phthalate is one of the commonly used phthalate esters in various plastics and consumer products. Dihexyl phthalate is classified as a priority pollutant and an endocrine disruptor. Dihexyl phthalate can induce reactive oxygen species (ROS) accumulation, promote inflammation, and lead to significant increases in apoptosis and inflammation-related gene expression levels. Dihexyl phthalate can cause testicular atrophy and is a reproductive toxicant .
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- HY-14742
-
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Opioid Receptor
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Others
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Faxeladol is a compound with analgesic activity that reduced mean pain intensity compared with placebo in a suppression trial for painful polyneuropathy with a favorable safety profile.
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-
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- HY-13219
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-
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- HY-13829
-
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HIV
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Infection
|
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BMS-585248 is a potent, third-generation HIV-1 attachment inhibitor with a promising initial in vitro and in vivo pharmacokinetic profile .
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-
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- HY-108609
-
-
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- HY-108711
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-
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- HY-123214
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Antibiotic
Bacterial
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Others
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Rifametane is a new 3-azamethyl-rifamycin with a pharmacokinetic profile superior to that of rifampin and activity with peak serum concentrations higher than that of rifampin in healthy volunteers.
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-
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- HY-P4062
-
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BIL
|
Insulin Receptor
|
Metabolic Disease
|
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Insulin peglispro (BIL) is a basal insulin with a flat, prolonged activity profile. Insulin peglispro can exhibit better glycaemic control compared to conventional insulins .
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- HY-W250743
-
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Biochemical Assay Reagents
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Others
|
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Cresyl diphenyl phosphate is a compound that disrupts lipid homeostasis in zebrafish embryos, causing alterations in lipid content and lipidomic profiles, as well as affecting gene expression and energy homeostasis. |
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-
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- HY-103491
-
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iGluR
|
Neurological Disease
|
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PF-06462894 is an alkyne-lacking metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator profiled in both rat and nonhuman primates .
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- HY-111199
-
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FAAH
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Neurological Disease
|
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JP83 is an irreversible fatty acyl amide hydrolase (FAAH) inhibitor with an IC50 of 1.6 nM in competitive activity-based protein profiling (ABPP) experiments .
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-
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- HY-145285
-
|
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Apelin Receptor (APJ)
|
Cardiovascular Disease
|
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APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease .
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- HY-N1798
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-
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- HY-145284
-
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Apelin Receptor (APJ)
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Cardiovascular Disease
|
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APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease .
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- HY-122620
-
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Hetrombopag (tautomerism); SHR-8735 (tautomerism)
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Thrombopoietin Receptor
|
Inflammation/Immunology
Cancer
|
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Rafutrombopag (tautomerism) is a potent thrombopoietin receptor agonist. Rafutrombopag (tautomerism) is efficacious and well tolerated with a manageable safety profile. Rafutrombopag (tautomerism) has the potential for the research of immune thrombocytopenia .
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- HY-109555
-
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HMR 1964
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Insulin Receptor
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Metabolic Disease
|
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Insulin glulisine (HMR 1964) is a rapid-acting insulin analogue, it mimics the pharmacokinetic and pharmacodynamic profiles of physiological human insulin. Insulin glulisine can be used for the research of diabetes .
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- HY-114301
-
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Sodium Channel
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Neurological Disease
|
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PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
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- HY-16421
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(-)-DRF 2725; NNC 61-0029
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PPAR
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Metabolic Disease
|
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Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic.
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- HY-144291
-
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Dopamine Receptor
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Neurological Disease
|
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LY3154885 is an orally active dopamine D1 receptor positive allosteric modulator (PAM). LY3154885 has an improved agent-agent interactions (DDI) risk profile .
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-
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- HY-156654
-
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PF-07817883
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SARS-CoV
Virus Protease
|
Infection
|
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Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CL pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 .
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- HY-118179
-
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mGluR
|
Neurological Disease
|
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VU0486321 is a compound in a class of mGlu1 positive allosteric modulators (PAMs). VU0486321 maintains acceptable mGlu1 PAM potency, DMPK profile, CNS permeability, and mGluR selectivity.
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- HY-117690
-
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PROTACs
Epigenetic Reader Domain
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Cancer
|
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dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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- HY-119926
-
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Hydroxylupanine
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Integrin
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Cardiovascular Disease
Neurological Disease
|
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13-Hydroxylupanine (Hydroxylupanine) is the typical alkaloid profile of sweet lupins.13-Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle .
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-
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- HY-135737
-
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Dioctyl carbonate
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Biochemical Assay Reagents
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Others
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Dicaprylyl carbonate, a solid, plant-derived fat, is a dry emollient. Dicaprylyl carbonate has excellent dermatological compatibility and a comprehensive performance profile, such as solubilizing and dispersing ability for sun-care filters .
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- HY-119926A
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Hydroxylupanine hydrochloride
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Others
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Cardiovascular Disease
Neurological Disease
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13-Hydroxylupanine Hydroxylupanine is the typical alkaloid profile of sweet lupins. 13-Hydroxylupanine Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle .
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- HY-114301A
-
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Sodium Channel
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Neurological Disease
|
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PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile .
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-
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- HY-168140
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-
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- HY-B2209B
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Vitamin B12a acetate
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Endogenous Metabolite
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Metabolic Disease
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Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia .
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-
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- HY-145362
-
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LPL Receptor
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Others
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S1P1 agonist 4 has a better profile in both potency (EC50 < 0.05 mg/kg) and predicted human half-life (t1/2 ∼ 5 days).
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-
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- HY-148739
-
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PROTACs
Epigenetic Reader Domain
|
Cancer
|
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dBRD 9-A is a PROTAC which can selective degrade BRD9. dBRD 9-A improves the bromine domain binding profile and reduces the binding activity of the whole BET family .
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- HY-119410
-
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HN11500
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Prostaglandin Receptor
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Cardiovascular Disease
|
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Linotroban (HN11500), a Sulotroban (HY-158332) derivative, is an orally active, potent non-prostanoid thromboxane receptor antagonist (TXRA) with a strong antiplatelet profile. Linotroban is used as antithrombotic agent .
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- HY-12883A
-
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Sodium Channel
|
Neurological Disease
|
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PF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771 .
|
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- HY-120802
-
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AZD-8871; LAS191351
|
mAChR
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Navafenterol (AZD-8871) is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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- HY-12352A
-
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STAT
Apoptosis
|
Cancer
|
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HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study .
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- HY-116524
-
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5-HT Receptor
|
Neurological Disease
|
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PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .
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- HY-14305A
-
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p38 MAPK
Autophagy
|
Inflammation/Immunology
|
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BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease .
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- HY-14312
-
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nAChR
|
Neurological Disease
|
|
A 85380 is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 exhibits selectivity for the α4β2 nAChR subtypes. A 85380 has a broad-spectrum analgesic profile .
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-
- HY-157132
-
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FAAH
|
Neurological Disease
|
FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity .
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- HY-161178
-
|
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Bacterial
|
Infection
|
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LK-60 is a potent DprE1 inhibitor. LK-60 effectively inhibits the proliferation of Mycobacterium tuberculosis. LK-60 has good safety profiles to gut microbiota and human cells .
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-
- HY-110131
-
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nAChR
|
Neurological Disease
|
|
A 85380 hydrochloride is a novel, high affinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .
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-
- HY-D1082
-
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Fluorescent Dye
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Others
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5-DTAF is a isomeric fluorescein derivative that directly react with polysaccharides and other alcohols in aqueous solution at pH ＞ 9. The maximum of the 5-DTAF emission profile is at a wavelength of 518 nm after excitation at 488 nm .
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- HY-101447A
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EPH 116 hydrochloride
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Estrogen Receptor/ERR
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Cancer
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SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
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- HY-W011053
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Taste Receptor
Apoptosis
Drug Derivative
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Others
Metabolic Disease
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Neotame is a derivative of Aspartame (HY-B0361) and is a flavor enhancer and low-caloric, non-nutritive, high-intensity artificial sweetener that is 7000-13,000 times sweeter than sugar. Neotame causes intestinal epithelial cell death at high concentrations. Neotame induces Apoptosis of Caco-2 cells .
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- HY-119402
-
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BCL6-IN-8c
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Bcl-2 Family
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Cancer
|
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TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in cell-free enzyme-linked immunosorbent assay .
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-
- HY-120802A
-
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AZD-8871 saccharinate; LAS191351 saccharinate
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mAChR
Adrenergic Receptor
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Infection
Inflammation/Immunology
|
|
Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile .
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- HY-B2209
-
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Vitamin B12a
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Endogenous Metabolite
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Metabolic Disease
|
|
Hydroxocobalamin (Vitamin B12a) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
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- HY-A0147
-
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OPC-17116; dl-Grepafloxacin
|
Antibiotic
Bacterial
|
Infection
|
|
Grepafloxacin (OPC-17116) is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin has high tissue penetration and a promising pharmacodynamic profile .
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- HY-A0147A
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OPC-17116 hydrochloride; dl-Grepafloxacin hydrochloride
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Antibiotic
Bacterial
|
Infection
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Grepafloxacin (OPC-17116) hydrochloride is an oral actively fluoroquinolone antibiotic with potent activity against community-acquired respiratory pathogens including Streptococcus pneumonia. Grepafloxacin hydrochloride has high tissue penetration and a promising pharmacodynamic profile .
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- HY-151524
-
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Cathepsin
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Inflammation/Immunology
|
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Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC50 value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies .
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- HY-155653
-
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BCRP
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Cancer
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ABCG2-IN-2 is a potent ABCG2 inhibitor with favorable oral pharmacokinetic profiles in mice. ABCG2-IN-2 can be used for the research of tumor multidrug resistance (MDR) and erythropoietic protoporphyria (EPP) .
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- HY-133145A
-
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NO Synthase
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Inflammation/Immunology
Cancer
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hDDAH-1-IN-2 is a selective, orally active human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1) inhibitor. hDDAH-1-IN-2 reveals an excellent profile regarding cell toxicity/viability .
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- HY-B2209A
-
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Vitamin B12a monohydrochloride
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Endogenous Metabolite
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Metabolic Disease
|
|
Hydroxocobalamin monohydrochloride (Vitamin B12a monohydrochloride) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
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- HY-133145
-
-
- HY-139708
-
|
|
iGluR
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Neurological Disease
|
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NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells.
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-
- HY-N7058A
-
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Endogenous Metabolite
|
Others
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Trans-Jasmone is a flavoring ingredient with aroma-inducing activity. Trans-Jasmone can be used as a fragrance agent to give products a unique aroma profile. Trans-Jasmone has potential biological activity and may be widely used in the flavoring and food industries .
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- HY-111021
-
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LPL Receptor
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Inflammation/Immunology
|
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ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
|
-
- HY-W751418
-
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(Z)-2-tetracos-15-enamidoethanesulfonic acid
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FAAH
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Neurological Disease
|
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N-Nervonoyl taurine ((Z)-2-tetracos-15-enamidoethanesulfonic acid) is a fatty acid-taurine conjugate derived from nervonic acid. N-Nervonoyl taurine is a substrate of fatty acid amide hydrolase (FAAH) discovered during metabolite profiling .
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- HY-111021A
-
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LPL Receptor
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Inflammation/Immunology
|
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ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile .
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- HY-163505
-
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Bacterial
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Others
|
|
Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
|
-
- HY-126943
-
|
|
Fluorescent Dye
|
Others
|
|
SAHA-BPyne is an activity-based protein profiling (ABPP) probe for detecting HDAC activity, which covalently labels the proximal proteins through a photoactivation. SAHA-BPyne inhibits HDAC activity in HeLa nuclear lysate with an IC50 of less than 5 μM .
|
-
- HY-15985A
-
|
|
Akt
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
CTX-0294885 hydrochloride is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 hydrochloride is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
|
-
- HY-15985
-
|
|
Akt
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
CTX-0294885 is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
|
-
- HY-105040
-
|
LY2140023 hydrate
|
mGluR
|
Neurological Disease
|
|
Pomaglumetad methionil (LY2140023 hydrate) is an oral methionine prodrug of the potent specific mGlu2/3 receptor agonist LY404039 (HY-50906). Pomaglumetad methionil is well-tolerated and has a distinct safety profile, and can be used for schizophrenia .
|
-
- HY-106588
-
|
SKI 2053R
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles .
|
-
- HY-169223
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
Roxatidine hydrochloride is an anti-ulcer compound with the activity of inhibiting gastric acid secretion. Roxatidine hydrochloride effectively inhibits duodenal and gastric ulcers and reduces ulcer pain. Roxatidine hydrochloride has a better safety profile than other similar compounds due to the lower dose required for effective inhibition .
|
-
- HY-13550A
-
|
NSC 196473 acetate; NSC 290813 acetate
|
DNA/RNA Synthesis
|
Cancer
|
|
Ametantrone acetate (NSC 196473 acetate) is an antineoplastic drug with topoisomerase II inhibitory activity. Ametantrone acetate causes covalent cross-linking of DNA. The pharmacokinetic profile of Ametantrone acetate has been confirmed in clinical trials, and its elimination pathway in the body indicates the existence of a major metabolic pathway .
|
-
- HY-N6861
-
|
|
Apoptosis
|
Cancer
|
|
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells .
|
-
- HY-149759
-
|
|
SHP2
ERK
|
Cancer
|
|
SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC50=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC50=5 nM .
|
-
- HY-114147
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Tuberculosis inhibitor 3 (compound 2i) displays potent anti-TB activity (MIC < 0.016 μg/mL) against agent-sensitive/resistant MTB strains. Tuberculosis inhibitor 3 (compound 2i) shows acceptable PK profiles with oral bioavailability .
|
-
- HY-103266
-
|
|
Aurora Kinase
|
Cancer
|
|
TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
|
-
- HY-13556
-
|
LY353381; SERM III
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile .
|
-
- HY-169916
-
|
|
Bacterial
Estrogen Receptor/ERR
|
Infection
|
|
GuaB-IN-1 (Compound 15) exhibits high potency against M.tb with a MIC value of 0.25 μM. GuaB-IN-1 has a favorable 28% hERG inhibition profile at 10 μM. GuaB-IN-1 is promising for research of tuberculosis .
|
-
- HY-15260C
-
|
BMS-863233 hydrochloride
|
CDK
|
Cancer
|
|
XL413 (BMS-863233) hydrochloride is an orally active and selective CDC7 inhibitor (IC50=3.4 nM). XL413 hydrochloride has favorable pharmacokinetic profiles and significantly inhibits tumor growth in rodent models. XL413 hydrochloride can be used in cancer research .
|
-
- HY-113603
-
|
SPR001; LY2371712
|
CRFR
|
Cancer
|
|
Tildacerfont is a potent and orally active corticotrophin-releasing factor type 1 (CRF1) receptort antagonis. Tildacerfont effectively reduces adrenocorticotropic hormone (ACTH) and adrenal androgen levels. Tildacerfont has favourable safety profile. Tildacerfont can be used for researching congenital adrenal hyperplasia .
|
-
- HY-139485
-
|
|
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
BMS-986224 is a potent, selective and orally active APJ receptor agonist (Kd = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1) apelin-13. BMS-986224 has the potential for the research of heart failure .
|
-
- HY-B2209BR
-
|
Vitamin B12a (acetate) (Standard)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxocobalamin (acetate) (Standard) is the analytical standard of Hydroxocobalamin (acetate). This product is intended for research and analytical applications. Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia .
|
-
- HY-134772
-
|
|
STAT
Cytochrome P450
|
Inflammation/Immunology
|
|
AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research .
|
-
- HY-170797
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-80 (Compound 10n) is a potent competitive inhibitor of α-glucosidase, with an IC50 of 48.4 μM. α-Glucosidase-IN-80 has good pharmacokinetic properties and toxicity profiles and can be used in the research of diabetes-related diseases .
|
-
- HY-138916
-
|
|
Biochemical Assay Reagents
EGFR
|
Others
|
|
PF-06672131 is an alkynylated afatinib derivative and a small molecule probe that is reactive to cysteine. PF-06672131 is an inhibitor of epidermal growth factor receptor (EGFR) kinase that targets the ATP pockets of EGFR. PF-06672131 can be used for activity-based protein profiling studies .
|
-
- HY-165069
-
|
Sphingomyelin (d18:1 C22:0)
|
Others
|
Others
|
|
N-Docosanoyl-D-erythro-sphingosylphosphorylcholine (Sphingomyelin (d18:1 C22:0)) is a compound that appears in the plasma sphingolipid profile after chronic hepatitis C virus infection. The level of this substance in plasma is associated with hepatic steatosis and may be an independent factor of hepatic steatosis.
|
-
- HY-108519
-
|
|
ROCK
|
Neurological Disease
|
|
AS1892802 is a potent, orally active, and highly selective inhibitor of ROCK. The onset of antinociceptive effect of AS1892802 is as fast as those of Tramadol and Diclofenac. AS1892802 did not induce gastric irritation or abnormal behavior. AS1892802 is an attractive analgesic profile for the research of severe osteoarthritis pain .
|
-
- HY-151100
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable .
|
-
- HY-115989
-
|
|
HCV
|
Infection
|
|
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
|
-
- HY-151561
-
|
|
Parasite
|
Infection
|
|
WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile .
|
-
- HY-143889
-
|
|
CDK
|
Cancer
|
|
Senexin C is a selective and orally active CDK8/19 inhibitor. Senexin C shows a strong tumor-enrichment pharmacokinetic (PK) profile and tumor-pharmacodynamic (PD) marker responses. Senexin C inhibits the growth of MV4-11 leukemia cells with good tolerability .
|
-
- HY-161029
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (Ki=22 nM, IC50=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .
|
-
- HY-162113
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 174 (Compound 5g) is a antibacterial agent. Antibacterial agent 174 has potent anti-infective potential in vivo and appreciable pharmacokinetic profiles. Highly active antibacterial agent 174 has favorable biofilm removal performance, low hemolysis and acceptable mammalian cell toxicity .
|
-
- HY-P4209A
-
|
|
Virus Protease
|
Others
|
|
Boc-GRR-AMC (TFA) is a tri-peptide Substrate. Boc-GRR-AMC can be used for a fluorogenic West Nile virus (WNV) substrate, profiling the substrate specificity for the NS2B-NS3 proteases or determining the pH optimum of LdMC activity .
|
-
- HY-145698
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
UCSF678 is a 42 nM arrestin-biased partial agonist at the 5-HT5AR with a more restricted off-target profile and decreased assay liabilities. UCSF678 is a selective probe with which to study the function of the 5-HT5AR .
|
-
- HY-P1112
-
-
- HY-145311
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Bis-Pro-5FU (Compound 4) is a 5-FU precursor that confers oral bioavailability and increase the safety profile of 5-Fluorouracil (5-FU) chemotherapy regimens. 5-FU is an antineoplastic antimetabolite that is widely used for the research of colorectal and pancreatic cancer .
|
-
- HY-125840
-
|
PT2977; MK-6482
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
|
-
- HY-B2209R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxocobalamin (Standard) is the analytical standard of Hydroxocobalamin. This product is intended for research and analytical applications. Hydroxocobalamin (Vitamin B12a) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
|
-
- HY-162822
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp modulator-5 (compound 25) is a modulator of P-gp and can inhibit the proliferation of multidrug resistant (MDR) tumors. P-gp modulator-5 inhibits the activity of drug efflux pumps in MDR cells, leading to a large accumulation of ROS and altered cell cycle profiles .
|
-
- HY-138800
-
|
|
nAChR
|
Neurological Disease
|
|
Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. Spinosad has an excellent environmental and mammalian toxicological profile. Larvicidal activity .
|
-
- HY-107784
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis .
|
-
- HY-155804
-
|
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
|
|
RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species .
|
-
- HY-P1112A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
|
-
- HY-130251
-
|
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
|
DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile .
|
-
- HY-152535
-
|
|
HSV
|
Infection
Inflammation/Immunology
|
|
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
|
-
- HY-159997
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
AD353 is a selective sigma-1 receptor ligand with antiallodynic activity. AD353 exhibits high potency both in a model of Capsaicin (HY-10448)-induced allodynia and in PGE2-induced mechanical hyperalgesia. AD353 exhibits a favorable pharmacokinetic profile .
|
-
- HY-112613
-
UCB9608
1 Publications Verification
|
PI4K
|
Inflammation/Immunology
|
|
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent .
|
-
- HY-120574
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
|
-
- HY-17552
-
|
Choline Alfoscerate; Alpha-GPC; L-α-GPC
|
Cholinesterase (ChE)
Endogenous Metabolite
|
Neurological Disease
|
|
sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia .
|
-
- HY-149982
-
-
- HY-146697
-
|
|
Trk Receptor
c-Fms
PDGFR
Bcr-Abl
c-Kit
Apoptosis
|
Cancer
|
|
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
|
-
- HY-15286
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Sodium 4-pentynoate is a alkynylacetate analogue, can be metabolically incorporated onto cellular proteins through biosynthetic mechanisms for profiling of acetylated proteins in diverse cell types . Sodium 4-pentynoate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-122051
-
AC1903
1 Publications Verification
|
TRP Channel
|
Metabolic Disease
|
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .
|
-
- HY-126248
-
|
|
PARP
|
Cancer
|
|
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model .
|
-
- HY-126321
-
|
|
ROR
|
Cancer
|
|
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy .
|
-
- HY-112081
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
|
-
- HY-N7539
-
|
|
Others
|
Metabolic Disease
|
|
Cognac oil, mainly found in wine lees, has unique fatty acid profiles, including Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), Oleic acid (8.3%) and other fatty acids. Cognac oil leads to a general increase in the permeation of R6G (Rhodamine 6G) across all the membranes .
|
-
- HY-B2209AR
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxocobalamin (monohydrochloride) (Standard) is the analytical standard of Hydroxocobalamin (monohydrochloride). This product is intended for research and analytical applications. Hydroxocobalamin monohydrochloride (Vitamin B12a monohydrochloride) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia .
|
-
- HY-18767
-
Ivosidenib
Maximum Cited Publications
11 Publications Verification
AG-120
|
Isocitrate Dehydrogenase (IDH)
|
Metabolic Disease
Cancer
|
|
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
|
-
- HY-147698
-
|
|
CDK
Topoisomerase
Apoptosis
|
Cancer
|
|
ZLHQ-5f is a dual CDK2 and Topo I inhibitor with an IC50 of 0.145 μM against CDK2/CycA2. ZLHQ-5f arrests the cell cycle in S-phase, triggers apoptosis in HCT116 cells, and has a good safety profile .
|
-
- HY-161316
-
|
|
Amine N-methyltransferase
|
Neurological Disease
Metabolic Disease
Cancer
|
|
NNMT-IN-5 (Compound 3-12) is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50 = 47.9 ± 0.6 nM). NNMT-IN-5 also has an excellent selectivity profile over a panel of human methyltransferases. NNMT-IN-5 can be used for the research of cancer, diabetes, metabolic disorders, and neurodegenerative diseases .
|
-
- HY-149940
-
|
|
SARS-CoV
|
Infection
|
|
SIMR3030 is a potent SARS-CoV-2 PLpro inhibitor with an IC50 value of 0.0399 µg/mL. SIMR3030 shows antiviral activity. SIMR3030 decreases SARS-CoV spike, ORF1b, IFN-α, IL-6 mRNA expression. SIMR3030 exhibits a satisfactory safety profile in mice .
|
-
- HY-119005A
-
-
- HY-132246
-
|
|
MAGL
|
Neurological Disease
|
|
WWL123 analogue-1 is an analogue of WWL123. WWL123 is a potent and selective ABHD6 inhibitor with an IC50 of 430 nM . WWL123 crosses the blood-brain-barrier and inhibits ABHD6 in brain parenchyma. ABHD6 blockade by WWL123 exerts an antiepileptic effect in Pentylenetetrazole (PTZ)-induced epileptiform seizures and spontaneous seizures in R6/2 mice .
|
-
- HY-16636
-
|
|
mGluR
|
Neurological Disease
|
|
ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile . ML337 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-106572A
-
|
|
Bacterial
|
Infection
|
|
Cefbuperazone sodium is an antibacterial agent that demonstrates significant activity against bacterial infections. Cefbuperazone sodium exhibits a linear pharmacokinetic profile, allowing for effective dosage determination in clinical settings. Cefbuperazone sodium reaches peak concentrations in human plasma following intravenous infusion, indicating its rapid absorption and distribution. Cefbuperazone sodium is primarily excreted unchanged in urine, highlighting its efficiency in renal elimination.
|
-
- HY-114237
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .
|
-
- HY-103193
-
|
Colforsin dapropate hydrochloride
|
Adenylate Cyclase
|
Cardiovascular Disease
|
|
NKH477 (Colforsin dapropate hydrochloride) directly activates the catalytic unit of adenylate cyclase and increases intracellular cAMP. NKH477 is a forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 exerts an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute rejection of rat orthotopic lung allografts .
|
-
- HY-16023B
-
|
EM-343; (Rac)-EM-652
|
Estrogen Receptor/ERR
|
Cancer
|
|
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor?antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380 .
|
-
- HY-147918
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 73 (compound CIB-3b) is a anticancer agent, potently targeting TAR RNA-binding protein 2 (TRBP) and disrupts its interaction with Dicer. Anticancer agent 73 can rebalance the expression profile of oncogenic or tumor-suppressive miRNAs. Anticancer agent 73 suppresses the proliferation and metastasis of HCC in vitro and in vivo .
|
-
- HY-158245
-
|
|
Acetolactate Synthase (ALS)
|
Others
|
|
Herbicide safener-2 (Compound III-7) is a herbicide safener with the same pharmacokinetic profile as the safener mefenpyr-diethyl (HY-136376). Herbicide safener-2 competitively binds to the acetolactate synthase (ALS) active site with mesosulfuron-methyl (HY-126987). Herbicide safener-2 protects crops against herbicide injury .
|
-
- HY-100375
-
|
ALKS 8700; BIIB098
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity .
|
-
- HY-P10707
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Tpp-CAQK can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK, with excellent bioactivity. Mito-Tpp-CAQK can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury .
|
-
- HY-155074
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-79 (compound 21) is an EGFR inhibior with antitumor activity. EGFR-IN-79 induces ROS-independent apoptosis and EGFR/AKT/mTOR-mediated autophagy. EGFR-IN-79 induces cell death at both proliferating and quiescent zones of EJ28 spheroids. EGFR-IN-79 exhibits safety profile in the zebrafish-based model .
|
-
- HY-162121
-
|
|
Others
|
Cancer
|
|
Antitumor agent-129 (Compound 68) is a thiazolidin-4-one sulfone derivative and an Osteosarcoma (OS) inhibitor with an IC50 value of 0.217 μM, a half-life of 73.8 min (mouse liver microsome) and an excellent pharmacokinetic profile (in vivo bioavailability F = 115%, intraperitoneal administration). Antitumor agent-129 is a potential candidate for OS research .
|
-
- HY-119530
-
|
BW 57-323
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-125384
-
|
|
Fluorescent Dye
|
Inflammation/Immunology
|
|
ARN14686 is an activity-based protein profiling (ABPP) probe. ARN14686 inhibits hNAAA with high potency (IC50=0.006 μM). ARN14686 interacts with NAAA via covalent binding to the N-terminal cysteine. ARN14686 binds only to the catalytically active form of NAAA, and may serve therefore as an efficient activity-based probe .
|
-
- HY-11048
-
NS11394
3 Publications Verification
|
GABA Receptor
|
Neurological Disease
|
|
NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties .
|
-
- HY-124754
-
|
BTRX-335140; CYM-53093
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
|
-
- HY-159081
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-20 (compound 3m) is an acetylcholinesterase (AChE, IC50=34.81 µM) and butylcholinesterase (BChE, IC50=20.66 µM) inhibitor, which has been demonstrated to have affinity for key enzyme pockets and favorable interaction profiles by molecular docking and kinetic simulations, and can be used in the study of Alzheimer's disease .
|
-
- HY-139562
-
|
|
FXR
|
Metabolic Disease
|
|
BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis .
|
-
- HY-143330
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
|
-
- HY-147547
-
|
|
Amyloid-β
|
Neurological Disease
|
|
SV5 is a potent anti-Alzheimer agent. SV5 can significantly protect SHSY-5Y cells against Aβ1-42-induced death. SV5 shows moderate antioxidant and good neuroprotective activities. SV5 shows the high stability in human plasma and the best pharmacological profile .
|
-
- HY-149014
-
|
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life .
|
-
- HY-P10707A
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Tpp-CAQK TAF can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK TFA, with excellent bioactivity. Mito-Tpp-CAQK TFA can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury .
|
-
- HY-153855
-
|
RXC004
|
Wnt
Acyltransferase
Porcupine
|
Cancer
|
|
Zamaporvint (RXC004) is an orally active and selective inhibitor of Wnt. Zamaporvint targete membrane-bound o-acyltransferase Porcupine and inhibited Wnt ligand palmitoylation, secretion, and pathway activation. Zamaporvint displays a favorable pharmacokinetic profile and shows potent antiproliferative effects in Wnt ligand-dependent colorectal and pancreatic cell lines. Zamaporvint possesses multiple antitumor mechanisms and can be used in cancer research .
|
-
- HY-12995A
-
|
|
FLAP
|
Inflammation/Immunology
|
|
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
|
-
- HY-151813
-
|
|
Fluorescent Dye
|
Cancer
|
|
NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
|
-
- HY-131914B
-
|
|
Sigma Receptor
|
Inflammation/Immunology
|
|
EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
|
-
- HY-N6652
-
|
Uracil 1-β-D-arabinofuranoside
|
Others
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties . 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells .
|
-
- HY-107784R
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Ectoine (Standard) is the analytical standard of Ectoine. This product is intended for research and analytical applications. Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis .
|
-
- HY-150654
-
|
|
WDR5
|
Cancer
|
|
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
|
-
- HY-162010
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-13 is a potent and orally active methionine adenosyltransferase 2A (MAT2A) inhibitor with a favorable pharmacokinetic profile.
MAT2A-IN-13 shows in vivo potency in an HCT-116 MTAP-deleted xenograft model. MAT2A-IN-13 can be used for MTAP-Deleted tumors treatment research .
|
-
- HY-151915
-
|
|
ATM/ATR
mTOR
|
Cancer
|
|
ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC50 of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC50 of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects .
|
-
- HY-149099
-
|
|
RET
|
Cancer
|
|
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
|
-
- HY-163468
-
|
|
Src
|
Cancer
|
|
SRC-3-IN-1 (compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor (IC50=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research .
|
-
- HY-138800R
-
|
|
nAChR
|
Neurological Disease
|
|
Spinosad (Standard) is the analytical standard of Spinosad. This product is intended for research and analytical applications. Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. Spinosad has an excellent environmental and mammalian toxicological profile. Larvicidal activity .
|
-
- HY-149844
-
|
|
Fungal
|
Infection
|
|
S-F24 is an antifungal agent with excellent broad-spectrum. S-F24 inhibits CYP3A4 with an IC50 value of 0.4 μM. S-F24 displays a good safety profile with high selectivity, low hemolytic effects, and low tendency to induce resistance. S-F24 can be used for research on fungal infections .
|
-
- HY-135303
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis . GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-113430
-
|
5-Heneicosylresorcinol
|
Fungal
|
Infection
|
|
5-n-Heneicosylresorcinol (5-Heneicosylresorcinol) is an active n-alkyl(enyl)resorcinols (AR) occurring in cereal products from Colombia. Antifungal activity .
|
-
- HY-122229
-
|
|
HIV
|
Infection
|
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-138657
-
|
|
Phosphatase
|
Cancer
|
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model .
|
-
- HY-170961
-
|
|
Aminopeptidase
Neprilysin
|
Neurological Disease
|
|
SDUY816 is an oral active dual APN/NEP inhibitor, with IC50 values of 0.68 μM for APN and 6.9 μM for NEP. SDUY816 exhibits analgesic effects and demonstrates good safety and pharmacokinetic profiles, with an oral bioavailability of 27% and a half-life of 4.02 hours in rats (oral administration, 10 mg/kg). SDUY816 has potential applications in the research of neuropathic pain disorders .
|
-
- HY-164041
-
|
|
PKC
|
Others
|
|
Staurosporine-Boc, a natural product isolated from the actinomyces Streptomyces staurosporeus, is a potent non-selective inhibitor of protein kinase. Staurosporine-Boc inhibits a variety of protein kinases, including protein kinase C (PKC), tyrosine kinase, and serine/threonine kinase. Because of its broad inhibition profile, Staurosporine-Boc is widely used as a tool compound in biological research, especially when studying cell signaling pathways .
|
-
- HY-137466
-
|
|
Topoisomerase
|
Cancer
|
|
ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research .
|
-
- HY-151933
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-49 is an orally active HIV-1 inhibitor, is a HEPT analog. HIV-1 inhibitor-49 possesses great pharmacokinetics profiles and potent non-nucleoside reverse transcriptase inhibitory activity (IC50=30 nM). HIV-1 inhibitor-49 exerts potential safety without acute toxicity in mouse model .
|
-
- HY-145294
-
|
|
ROCK
|
Neurological Disease
|
|
ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation .
|
-
- HY-115839
-
|
Tachmalcor free base
|
Sodium Channel
|
Others
|
|
Detajmium (Tachmalcor free base) is a Na?-channel blocker with activity to inhibit ventricular conduction and refractoriness. Detajmium (0.3μM) prolongs intraventricular conduction time comparable to propafenone (0.3μM) during sinus rhythm, but the time constant for reaching steady state during rapid ventricular pacing is significantly longer for Detajmium, indicating a unique temporal profile for its heart rate-dependent effects.
|
-
- HY-165119
-
|
PE(18:0/20:5); 18:0/20:5-PE
|
Endogenous Metabolite
|
Others
|
|
1-Stearoyl-2-eicosapentaenoyl-sn-glycero-3-PE (PE(18:0/20:5)) is a phospholipid identified in plasma lipid profile analysis, with similar lipid level changes in high-grade cervical intraepithelial neoplasia and cervical cancer compared with normal state and low-grade cervical intraepithelial neoplasia, and can be used to monitor cervical cancer progression.
|
-
- HY-150550
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile .
|
-
- HY-151424
-
|
|
Proteasome
|
Cancer
|
|
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
|
-
- HY-133870
-
|
ITalk
|
Fluorescent Dye
|
Inflammation/Immunology
|
|
Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate . Itaconate-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-125279
-
|
|
Parasite
|
Inflammation/Immunology
|
|
OAT-2068 is a selective, high activity and orally active inhibitor of mouse chitotriosidase (mCHIT1) (IC50=29 nM) and displays 143-fold selectivity over m AMCase (IC50=4170 nM). OAT-2068 displays a good pharmacokinetic profile and is an ideal tool to study the role of CHIT1 in biological systems, including animal models of human diseases .
|
-
- HY-150023
-
|
|
EGFR
Itk
PI4K
Btk
CDK
Raf
JAK
|
Cancer
|
|
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
|
-
- HY-A0087
-
|
|
Biochemical Assay Reagents
PPAR
Estrogen Receptor/ERR
Cytochrome P450
|
Others
|
|
Octocrylene is an organic ultraviolet (UV) filter that absorbs mainly UVB radiation and shorter UVA wavelengths. Octocrylene acts as a partial agonist of PPARγ, which alters the gene transcription profile of lipid metabolism enzymes. In addition, Octocrylene is cytotoxic and genotoxic to human skin fibroblasts and mediates the biosynthesis of estrogens such as estriol in zebrafish larvae, while affecting antioxidant pathways including glutathione transferase and peroxisomes .
|
-
- HY-131335
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
|
-
- HY-155518
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK4-IN-25 (compound 38) is an orally acitve and potent IRAK4 inhibitor (IC50=7.3 nM), with low clearance (Cl=12 mL/min/kg). IRAK4-IN-25 inhibits production of pro-inflammatory cytokines, and shows in vitro safety and ADME profiles. IRAK4-IN-25 can be used for research in inflammatory and autoimmune disorders .
|
-
- HY-124364
-
|
|
HBV
Cytochrome P450
|
Infection
Metabolic Disease
|
|
RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation .
|
-
- HY-155489
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
|
-
- HY-N7921
-
|
|
Bacterial
|
Others
|
|
Urolithin M6 is a polyhydroxy-rich metabolite with potential antioxidant activity. Urolithin M6 is produced by intestinal microbial metabolism and may act as an analog of tannic acid compounds. The production of Urolithin M6 in humans requires specific bacterial 3-dehydroxylase activity, which provides a new mechanism for its biotransformation. The metabolic profile of Urolithin M6 helps to stratify volunteers and further explore its potential role in health and disease .
|
-
- HY-P99625
-
|
SAR441344; INX-021
|
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Frexalimab (SAR441344) is a second-generation monoclonal antibody targeting the CD40 ligand (CD40L) with a good safety profile. Frexalimab inhibits the binding between CD40 and CD40L to modulate immune response. Frexalimab is likely to help prevent the process of β-cell destruction. Frexalimab is proming for multiple sclerosis, lupus erythematosus, Sjögren’s syndrome and type I diabetes research .
|
-
- HY-128656
-
|
|
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders .
|
-
- HY-137464A
-
OATD-01
1 Publications Verification
|
Others
|
Inflammation/Immunology
|
|
OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
|
-
- HY-155992
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
|
-
- HY-156793
-
|
|
PKC
|
Others
|
|
hRIO2 kinase ligand-1 (com 9) is a ligand of hRIO2 kinase, with a Kd value of 520 nM .
|
-
- HY-111755
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders .
|
-
- HY-150680
-
|
|
SARS-CoV
Histone Methyltransferase
DNA Methyltransferase
|
Infection
|
|
SARS-CoV-2 nsp14-IN-1 (Compound 3) is a prototypic bisubstrate inhibitor of SARS-CoV-2 Nsp14 MTase with an IC50 value of 0.061 μM. SARS-CoV-2 nsp14-IN-1 (Compound 3) has an excellent selectivity profile over a panel of human methyltransferases, can against apanel of 10 human MTases including histone lysine, proteinarginine, and DNA and RNA MTases .
|
-
- HY-162962
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1/TDO-IN-7 (Compound 43b), an isoquinoline derivative, is a potent dual IDO1/TDO inhibitor, with IC50s of 0.31 μM and 0.08 μM, respectively. IDO1/TDO-IN-7 displays acceptable pharmacokinetic profiles and potent antitumor efficacy with low toxicity in B16-F10 tumor model .
|
-
- HY-139602
-
|
|
Flavivirus
Dengue Virus
Virus Protease
|
Infection
|
|
(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models .
|
-
- HY-105048A
-
|
|
Bacterial
|
Infection
|
|
Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
|
-
- HY-136205
-
|
Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide
|
TRP Channel
|
Infection
Inflammation/Immunology
|
|
IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection . IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling . IA-Alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-119821R
-
|
|
Glycosidase
|
Infection
|
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
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- HY-157928
-
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Keap1-Nrf2
|
Inflammation/Immunology
|
|
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
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-
- HY-126250
-
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Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
|
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NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death . NPD-1335 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-119530R
-
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Nucleoside Antimetabolite/Analog
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Others
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Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
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-
- HY-136576
-
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LPL Receptor
Drug Metabolite
|
Inflammation/Immunology
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|
RP101075, an active metabolite of Ozanimod, is a potent, orally active S1PR (sphingosine-1-phosphate receptor 1) agonist, with an EC50 of 0.27 nM. RP101075 displays >100-fold selectivity over S1PR5 (EC50=5.9 nM) and >10000-fold over S1PR 2, 3, and 4. RP101075 displays superior cardiovascular safety profile .
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-
- HY-10063
-
|
TC-1734; ACD3480
|
nAChR
|
Neurological Disease
|
|
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
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-
- HY-130609
-
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γ-secretase
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Neurological Disease
|
|
Aβ42-IN-1, compound 1v, is a novel, potent and orally active?γ-secretase modulator (GSM). Aβ42-IN-1 potently reduced Aβ42 levels with an IC50?value of 0.091?μM without CYP3A4 inhibition. Aβ42-IN-1 shows a sustained pharmacokinetic profile.
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- HY-151872
-
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HDAC
Ferroptosis
|
Cancer
|
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HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-17552S
-
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Choline Alfoscerate-d9; Alpha-GPC-d9; L-α-GPC-d9
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
Endogenous Metabolite
|
Neurological Disease
|
|
sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
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-
- HY-125881
-
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LPL Receptor
|
Inflammation/Immunology
|
|
ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile .
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-
- HY-120965
-
|
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Endogenous Metabolite
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Metabolic Disease
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|
Several different arachidonoyl amino acids, including N-arachidonoyl dopamine (NADA) and N-arachidonoyl serine (ARA-S), have been isolated and characterized from bovine brain.1 During mass spectral lipidomic analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, is discovered. N-Palmitoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling. Its function is currently under investigation.
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-
- HY-117087
-
|
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Phosphatase
|
Cancer
|
|
K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
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-
- HY-155726
-
|
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Others
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Others
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Cy-FBP/SBPase-IN-1 (compound S5) is a Cy-FBP/SBPase inhibitor, which is an important regulatory enzyme in cyanobacterial photosynthesis. Thus Cy-FBP/SBPase-IN-1 inhibits Calvin cycle and photosystem, and decreases photosynthetic efficiency in cyanobacterial photosynthesis. Cy-FBP/SBPase-IN-1 potently inhibits the growth of cyanobacteria, as well as Synechocystis sp.PCC6803. Cy-FBP/SBPase-IN-1 shows safety profile in human-derived cells and zebrafish models .
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-
- HY-144437
-
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TGF-β Receptor
|
Cancer
|
|
ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .
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-
- HY-167734
-
|
AY-30715
|
COX
|
Inflammation/Immunology
|
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Pemedolac (AY-30715) is a potent analgesic with significant pain-relief efficacy against chemically induced and inflammatory pain in animal models. Pemedolac displays a notable separation between analgesic effects and anti-inflammatory activity, achieving effective pain relief at much lower doses than those required for anti-inflammatory or gastric irritant effects. Pemedolac also shows low ulcerogenic potential, indicating a safer profile compared to standard NSAIDs while being utilized for the treatment of neurological, skin, and musculoskeletal disorders.
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-
- HY-103006
-
NAI-N3
5 Publications Verification
|
Biochemical Assay Reagents
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Others
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NAI-N3 is a RNA acylation reagent that enables RNA purification. NAI-N3 is a dual-function SHAPE (selective 2-hydroxyl acylation and profiling experiment) probe (RNA structure probe and enrichment) . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
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-
- HY-146372
-
|
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CXCR
|
Cancer
|
|
CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately .
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-
- HY-108417
-
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STAT
JAK
Bcr-Abl
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Cancer
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|
Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
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-
- HY-101144
-
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TCD-717
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Others
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Cancer
|
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
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-
- HY-136528
-
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Deubiquitinase
Apoptosis
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Cancer
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RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells .
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-
- HY-14330
-
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Dopamine Receptor
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Neurological Disease
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ABT-724 is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
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-
- HY-147955
-
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Carbonic Anhydrase
Cholinesterase (ChE)
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Neurological Disease
Metabolic Disease
|
|
hCAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase isoenzymes I and II) inhibitor, with IC50 values of 37.88 and 45.23 nM, respectively. hCAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. hCAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
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-
- HY-111011
-
|
JNJ 38488502 acetate; FE 200665 acetate
|
Opioid Receptor
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Neurological Disease
|
|
CR 665 (JNJ 38488502) acetate is a kappa-opioid agonist that may effectively treat visceral pain by activating receptors on afferent nerves within the gut. CR 665 acetate exhibits peripheral selectivity, differentiating its pharmacokinetic profile from that of non-selective opioids like oxycodone. CR 665 acetate has demonstrated a beneficial effect on visceral pain tolerance thresholds without the delayed analgesic response characteristic of opioids that penetrate the brain. CR 665 acetate is proposed for use in managing postoperative pain due to its pain-relieving properties.
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-
- HY-114947
-
|
9-Deoxy-9-methylene PGE2
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Prostaglandin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
9-deoxy-9-methylene Prostaglandin E2 (9-deoxy-9-methylene PGE2) is a stable, isosteric analog of PGE2. 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at the same potency as PGE2.
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-
- HY-N6652R
-
|
|
Others
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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|
1-beta-D-Arabinofuranosyluracil (Standard) is the analytical standard of 1-beta-D-Arabinofuranosyluracil. This product is intended for research and analytical applications. 1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties . 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells .
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-
- HY-103409
-
|
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Dopamine Receptor
|
Neurological Disease
|
|
ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
|
-
- HY-16469
-
|
|
Akt
|
Cancer
|
|
SR13668 is a potent indole analog derived from indole-3-carbinol (I3C), known for its natural anticancer properties but limited by poor metabolic characteristics. Developed to enhance I3C's anticancer efficacy, SR13668 effectively inhibits growth factor-stimulated Akt activation. It demonstrates strong oral anticancer activity across different cancer types in preclinical studies, showing promise in clinical development due to its favorable safety profile and potent therapeutic effects .
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-
- HY-146353
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-29 (compound 14d2) is a potent HIV-1 inhibitor with an EC50 of 2.18 μM for HIV-1 IIIB. HIV-1 inhibitor-29 has high anti-resistance profile toward F227L/V106A strain (EC50 = 0.974 μM), and exhibits low cytotoxicity in MT-4 cells (CC50 = 211 μM). HIV-1 inhibitor-29 can be used for researching AIDS .
|
-
- HY-120964
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Several different arachidonoyl amino acids, including N-arachidonoyl dopamine (NADA) and N-arachidonoyl serine (ARA-S), have been isolated and characterized from bovine brain.1 During mass spectral lipidomic analysis of rat brain, a series of fatty acyl amides of a third amino acid, taurine, is discovered.2 This novel class of compounds is present in kidney and activates members of the transient receptor potential (TRP) family of calcium channels.3 N-Stearoyl taurine is a prominent amino-acyl endocannabinoid isolated from rat brain during lipidomics profiling.
|
-
- HY-144122
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-15 (compound 9d) is a highly potent and broad-spectrum HIV-1 inhibitor. HIV-1 inhibitor-15 has inhibitory activity against HIV-1 WT, L100I, K103N, Y181C, E138K with EC50s of 1.7 nM, 4 nM, 2 nM, 6 nM and 9 nM, respectively. HIV-1 inhibitor-15 has good solubility, safety profiles and favorable oral bioavailability .
|
-
- HY-115004
-
|
|
FAAH
|
Neurological Disease
|
|
MM-433593 is a potent and selective inhibitor of fatty acid amide hydrolase-1 (FAAH-1) that is orally administered to inhibit pain, inflammation, and related disorders. Pharmacokinetic studies of MM-433593 in macaques revealed a biphasic elimination profile with a rapid distribution phase and a slower elimination phase, with a systemic clearance of 8-11 mL/min/kg. MM-433593 exhibits moderate oral bioavailability (14-21%) and its metabolism primarily involves oxidation of the methyl group on the indole ring, resulting in a variety of sulfate, glucuronide, or glutathione-conjugated metabolites .
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-
- HY-101196
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
PG 9 maleate is a compound with analgesic and anti-memory loss activity. PG 9 maleate exerts analgesic effects by enhancing central cholinergic transmission. PG 9 maleate protects against memory loss caused by scopolamine or dicyclomine within a specific dose range. The affinity profile of PG 9 maleate indicates significant selectivity among the M4/M1 receptor subtypes, which may be the mechanism for its analgesic and anti-memory loss effects. PG 9 maleate can increase the release of acetylcholine, thereby improving its biological activity .
|
-
- HY-147954
-
|
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
|
α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy .
|
-
- HY-151156
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
|
-
- HY-139792
-
|
SHR117887
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Besigliptin tosylate (SHR117887) is a DPP-4 inhibitor with activity to improve metabolic control and β-cell function. Besigliptin tosylate can effectively reduce serum DPP-4 activity and improve oral glucose tolerance. Besigliptin tosylate significantly reduces fasting blood glucose levels and improves lipid profiles in a diabetic mouse model. The effect of besigliptin tosylate is comparable to that of the known compound vildagliptin (HY-14291) at the same concentration. Besigliptin tosylate increases insulin staining of pancreatic islet cells in chronic administration, indicating improved β-cell function .
|
-
- HY-151161
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-8 (compound 34) is a EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-8 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.45, 0.244 and 5.669 μM, respectively. EGFR/HER2-IN-8 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer .
|
-
- HY-162585
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs .
|
-
- HY-147319
-
|
|
Others
|
Neurological Disease
|
|
RTI-7470-44 is a potent, selective and blood-brain barrier (BBB) penetrant human trace amine-associated receptor subtype 1 (hTAAR1) antagonist with an IC50 value of 8.4 nM and a Ki value of 0.3 nM. RTI-7470-44 has moderate metabolic stability, and a favorable preliminary off-target profile. RTI-7470-44 can increase the spontaneous firing rate of mouse ventral tegmental area (VTA) dopaminergic neurons. RTI-7470-44 can be used for researching schizophrenia, agent addiction, and Parkinson’s disease (PD) .
|
-
- HY-155517
-
|
|
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
|
|
INF200 (compound 5) is a sulfonylurea-based inhibitor of NLRP3 and NLRP3-mediated pyroptosis. INF200 has beneficial cardiometabolic effects in rat model of high-fat diet (HFD)-induced metaflammation，and shows anti-inflammatory activity to (10 μM) decreases IL-1β release in human macrophages. INF200 improves glucose and lipid profiles，and attenuates systemic inflammation and biomarkers of cardiac dysfunction (particularly BNP). INF200 also improves myocardial damage-dependent ischemia/reperfusion injury (IRI) in hemodynamic evaluation .
|
-
- HY-10812
-
|
|
PI3K
mTOR
|
Cancer
|
|
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
|
-
- HY-149008
-
|
|
Amylases
|
Metabolic Disease
Cancer
|
|
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
|
-
- HY-124322
-
|
|
Beta-secretase
|
Neurological Disease
Inflammation/Immunology
|
|
NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
|
-
- HY-P99116
-
|
RG7716
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
|
-
- HY-161727
-
|
|
P2Y Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis .
|
-
- HY-14362
-
|
|
ROCK
Ribosomal S6 Kinase (RSK)
|
Cardiovascular Disease
|
|
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) .
|
-
- HY-170958
-
|
|
Src
Apoptosis
|
Cancer
|
Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
|
-
- HY-167939
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
(R)-Bambuterol is a β2-receptor agonist with anti-asthmatic and colitis-improving activity. (R)-Bambuterol is indicated for the treatment of asthma and chronic obstructive pulmonary disease and has the advantage of a once-daily dosing and a favorable side effect profile. (R)-Bambuterol significantly reduced disease severity in a mouse model of colitis, more effectively than (RS)-Bambuterol or (S)-Bambuterol. (R)-Bambuterol can significantly reduce the levels of inflammatory cytokines and reduce the infiltration of macrophages in mice with colitis. (R)-Bambuterol also increases β2-adrenoceptor levels and reduces the expression of IL-6, IL-17 and other related proteins in colon tissue in a dose-dependent manner .
|
-
- HY-P0037
-
|
Org 30850ANT
|
Others
GnRH Receptor
|
Endocrinology
|
|
Org-30850 is a potent LHRH antagonist designed for treating hormone-dependent disorders. In animal studies, a single subcutaneous dose effectively inhibited ovulation in rats and significantly reduced testosterone levels in male rats for up to 48 hours post-administration. Daily doses of Org-30850 in female rats suppressed estrous cycles, decreased uterine and ovarian weights, and lowered estradiol and FSH serum levels. In male rats, prolonged treatment resulted in reversible reductions in gonadal function and testosterone levels, with almost complete recovery observed after cessation of treatment. Unlike comparable LHRH antagonists, Org-30850 exhibited minimal injection site irritation and no edematous reactions, suggesting a more favorable therapeutic profile .
|
-
- HY-155297
-
|
FLA-136
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
|
-
- HY-101448
-
|
WAY-171318
|
MMP
Apoptosis
Interleukin Related
TNF Receptor
Caspase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TMI-1 (WAY-171318) inhibits TNF converting enzyme (TACE) (IC50 of 8.4 nM), ADAM-TS-4, ADAM-17 and various MMPs with oral activity. TMI-1 significantly suppresses the secretion of TNF-α , alleviating collagen-induced arthritis in mice. TMI-1 inhibits cancer cell proliferation, induces apoptosis through a caspase-dependent pathway. TMI-1 also reverses TRPV1 upregulation and lowers the levels of inflammatory factors (TNF-α、IL-1β、IL-6) in nerve cells, protecting against paclitaxel-induced neurotoxicity. TMI-1 leads to changes in pro-atherogenic lipoprotein profiles, but does not affect the progression of early lesions .
|
-
- HY-150537
-
|
|
Cholinesterase (ChE)
GSK-3
Microtubule/Tubulin
ROS Kinase
|
Neurological Disease
|
|
AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
|
-
- HY-30004
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
- HY-30004R
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
1-Aminocyclopropane-1-carboxylic acid (Standard) is the analytical standard of 1-Aminocyclopropane-1-carboxylic acid. This product is intended for research and analytical applications. 1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
-
-
HY-L0091V
-
|
|
1,367,511 compounds
|
|
Chemspace Lead-Like Compound Library contains 1,367,511 in-Stock lead-like compoundswith favorable physicochemical profiles and high Quantitative Estimation of Drug-likeness.
|
-
-
HY-L0093V
-
|
|
10,119 compounds
|
|
Diversity-based screening continues to be a vital tool for drug discovery. Efficiency and productivity can be improved by using screening libraries that offer maximum diversity whilst retaining drug-like properties. Chemspace Scaffold derived set composes 10,119 compounds, which including 3,373 scaffolds, 3 compounds per each. This library has exceptional coverage of drug-like chemical space.
|
-
-
HY-L021L
-
|
|
43 compounds
|
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE provides a unique collection of 43 natural product-like compounds that are structurally like Steroids, Tannins, Flavonoids, Quinones, Isoquinolines, etc. This library is an important source of lead compounds for drug discovery.
|
-
-
HY-L198
-
|
|
117 compounds
|
|
Unlike the 20 natural amino acids commonly found within living organisms, non-natural amino acids are synthesized through chemical or biosynthetic methods, thereby being endowed with unique chemical properties or biological activities. In drug development, these amino acids can be utilized to design novel pharmaceutical molecules that may exhibit superior pharmacological characteristics, such as increased selectivity, improved pharmacokinetic profiles, or reduced toxicity. In biomedical research, uon-natural amino acids can act as biological markers or probes for investigating biological processes like cell signaling, protein conformation, and protein-protein interactions. In addition, non-natural amino acids can also be used in the field of agriculture to develop new pesticides, plant growth regulators and so on.
|
-
-
HY-L0121V
-
|
|
10,000 compounds
|
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 10K Natural Product-like Compound Library consists of 10,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
|
-
-
HY-L905
-
|
|
5,000 compounds
|
|
Natural products are an attractive source with varied structures that exhibit potent biological activities, and desirable pharmacological profiles. The core scaffold of a natural product can also provide a biologically validated framework upon which to display diverse functional groups. Inspired by bioactive natural products, natural product-like compounds, occupying the same chemical space, are ideally suited to explore and to facilitate understanding of biological pathways.
MCE 5K Natural Product-like Compound Library consists of 5,000 natural product-like compounds. Each compound has scaffold of natural products or Tanimoto coefficient >0.6 with natural products. The natural-likeness scoring of these compounds is >-2. What’s more, compounds in the library are drug-like and readily available for re-supply, making it a powerful tool for new drug research and development. It can be widely applied in high-throughput screening (HTS) and high-content screening (HCS).
|
-
-
HY-L192
-
|
|
68 compounds
|
|
Dietary supplement, also known as nutritional supplement or food supplement, include dietary components such as vitamins, minerals, and amino acids. The unique value of dietary supplement is particularly significant in the post-pandemic era. Compared to traditional medication, dietary supplement is often more readily accepted by the public due to their higher safety profile and the natural origin. By orally supplementing essential nutrients and bioactive substances, dietary supplement can help to enhance the body's health level and reduce the risk of diseases. For certain chronic conditions, proper dietary supplement can also serve as a powerful adjunct to conventional medical treatment, enhancing the effectiveness of medication.
MCE has included 68 dietary supplements, whose ingredients are all derived from the official lists published by authoritative organizations such as the FDA, EFSA, NMPA, etc. These compounds can be utilized in the development of health food products and for the mechanistic research of certain chronic diseases.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D1082
-
|
|
Fluorescent Dyes/Probes
|
|
5-DTAF is a isomeric fluorescein derivative that directly react with polysaccharides and other alcohols in aqueous solution at pH ＞ 9. The maximum of the 5-DTAF emission profile is at a wavelength of 518 nm after excitation at 488 nm .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W075766
-
|
Nickel difluoride
|
Biochemical Assay Reagents
|
|
Nickel(II) fluoride (Nickel difluoride) is a fluorinating agent and catalyst suitable for surface treatment of aluminum profiles and the production of inks, fluorescent lamps, and organic synthesis. Nickel(II) fluoride is a kind of biological materials or organic compounds that are widely used in life science research .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-109555
-
|
HMR 1964
|
Insulin Receptor
|
Metabolic Disease
|
|
Insulin glulisine (HMR 1964) is a rapid-acting insulin analogue, it mimics the pharmacokinetic and pharmacodynamic profiles of physiological human insulin. Insulin glulisine can be used for the research of diabetes .
|
-
- HY-P10707A
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Tpp-CAQK TAF can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK TFA, with excellent bioactivity. Mito-Tpp-CAQK TFA can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury .
|
-
- HY-P4062
-
|
BIL
|
Insulin Receptor
|
Metabolic Disease
|
|
Insulin peglispro (BIL) is a basal insulin with a flat, prolonged activity profile. Insulin peglispro can exhibit better glycaemic control compared to conventional insulins .
|
-
- HY-P4209
-
|
|
Peptides
|
Others
|
|
Boc-GRR-AMC is a tri-peptide Substrate. Boc-GRR-AMC can be used for a fluorogenic West Nile virus (WNV) substrate, profiling the substrate specificity for the NS2B-NS3 proteases or determining the pH optimum of LdMC activity .
|
-
- HY-P4209A
-
|
|
Virus Protease
|
Others
|
|
Boc-GRR-AMC (TFA) is a tri-peptide Substrate. Boc-GRR-AMC can be used for a fluorogenic West Nile virus (WNV) substrate, profiling the substrate specificity for the NS2B-NS3 proteases or determining the pH optimum of LdMC activity .
|
-
- HY-P1112
-
-
- HY-P1112A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
|
-
- HY-P10707
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Tpp-CAQK can bind to mitochondria, enabling the construction of an engineered mitochondrial compound, Mito-Tpp-CAQK, with excellent bioactivity. Mito-Tpp-CAQK can be internalized by macrophages, thereby enhancing the phagocytosis of myelin debris, alleviating mitochondrial dysfunction, and reducing proinflammatory profiles, ultimately facilitating tissue repair and functional recovery in mice after spinal cord injury .
|
-
- HY-105048A
-
|
|
Bacterial
|
Infection
|
|
Omiganan pentahydrochloride is a cationic peptide compound with a broad antibacterial profile. Omiganan pentahydrochloride is capable of inhibiting a variety of bacteria, including yeast, and is active against both gram-positive and gram-negative bacteria. Omiganan pentahydrochloride is able to interact with the bacterial cell membrane, causing the destruction of the cell membrane and the death of the bacteria. Omiganan pentahydrochloride can be used for the study of antimicrobial activity against pathogens commonly associated with catheter-associated infections, including strains with drug-resistant phenotypes .
|
-
- HY-P0037
-
|
Org 30850ANT
|
Peptides
GnRH Receptor
|
Endocrinology
|
|
Org-30850 is a potent LHRH antagonist designed for treating hormone-dependent disorders. In animal studies, a single subcutaneous dose effectively inhibited ovulation in rats and significantly reduced testosterone levels in male rats for up to 48 hours post-administration. Daily doses of Org-30850 in female rats suppressed estrous cycles, decreased uterine and ovarian weights, and lowered estradiol and FSH serum levels. In male rats, prolonged treatment resulted in reversible reductions in gonadal function and testosterone levels, with almost complete recovery observed after cessation of treatment. Unlike comparable LHRH antagonists, Org-30850 exhibited minimal injection site irritation and no edematous reactions, suggesting a more favorable therapeutic profile .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P9989
-
|
REGN5458
|
CD3
TNF Receptor
|
Cancer
|
|
Linvoseltamab is a bispecific antibody targeting to both BCMA (TNFRSF17) and CD3 epsilon. Linvoseltamab shows safety profile and encouraging efficacy in relapsed/refractory multiple myeloma (RRMM) models .
|
-
- HY-P99625
-
|
SAR441344; INX-021
|
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Frexalimab (SAR441344) is a second-generation monoclonal antibody targeting the CD40 ligand (CD40L) with a good safety profile. Frexalimab inhibits the binding between CD40 and CD40L to modulate immune response. Frexalimab is likely to help prevent the process of β-cell destruction. Frexalimab is proming for multiple sclerosis, lupus erythematosus, Sjögren’s syndrome and type I diabetes research .
|
-
- HY-P99116
-
|
RG7716
|
VEGFR
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Faricimab, an overall good safety and tolerability profile, is a bispecific antibody targeting Angiopoietin-2 (Ang-2) and vascular endothelial growth factor-A (VEGF-A). Faricimab prevents retinal vascular leakage, cell death and inflammation in retinal ischemia/reperfusion (I/R) injury and sCNV mouse models. Faricimab demonstrates statistically superior visual acuity gains versus Ranibizumab (HY-P9951). Faricimab can be used for retinal diseases, such as age-related macular degeneration (w-AMD), diabetic macular edema (DME) and macular edema following retinal vein occlusion (RVO) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N2842
-
-
-
- HY-W005178
-
-
-
- HY-W011215
-
-
-
- HY-135737
-
-
-
- HY-B2209B
-
-
-
- HY-B2209
-
-
-
- HY-B2209A
-
-
-
- HY-W052051
-
-
-
- HY-N1798
-
-
-
- HY-119926A
-
-
-
- HY-W751418
-
-
-
- HY-N6861
-
-
-
- HY-B2209BR
-
|
Vitamin B12a (acetate) (Standard)
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
|
|
Hydroxocobalamin (acetate) (Standard) is the analytical standard of Hydroxocobalamin (acetate). This product is intended for research and analytical applications. Hydroxocobalamin acetate is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the research of vitamin B12 deficiency including pernicious anemia .
|
-
-
- HY-B2209R
-
-
-
- HY-138800
-
-
-
- HY-107784
-
-
-
- HY-17552
-
-
-
- HY-N7539
-
-
-
- HY-B2209AR
-
-
-
- HY-N6652
-
-
-
- HY-107784R
-
|
|
Structural Classification
Microorganisms
Source classification
Amino acids
|
Bacterial
|
|
Ectoine (Standard) is the analytical standard of Ectoine. This product is intended for research and analytical applications. Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis .
|
-
-
- HY-138800R
-
|
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
nAChR
|
|
Spinosad (Standard) is the analytical standard of Spinosad. This product is intended for research and analytical applications. Spinosad, a mixture of spinosyns A and D known as fermentation products of a soil actinomycete (Saccharopolyspora spinosa), is a biological neurotoxic insecticide with a broader action spectrum. Spinosad targets the nicotinic acetylcholine receptor (nAChRs) of the insect nervous system. Spinosad has an excellent environmental and mammalian toxicological profile. Larvicidal activity .
|
-
-
- HY-N7921
-
|
|
Structural Classification
Monophenols
Source classification
Phenols
Endogenous metabolite
|
Bacterial
|
|
Urolithin M6 is a polyhydroxy-rich metabolite with potential antioxidant activity. Urolithin M6 is produced by intestinal microbial metabolism and may act as an analog of tannic acid compounds. The production of Urolithin M6 in humans requires specific bacterial 3-dehydroxylase activity, which provides a new mechanism for its biotransformation. The metabolic profile of Urolithin M6 helps to stratify volunteers and further explore its potential role in health and disease .
|
-
-
- HY-119821R
-
|
|
Structural Classification
Microorganisms
Source classification
Phenols
Polyphenols
|
Glycosidase
|
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
-
- HY-N6652R
-
|
|
Structural Classification
Natural Products
Animals
Source classification
|
Others
|
|
1-beta-D-Arabinofuranosyluracil (Standard) is the analytical standard of 1-beta-D-Arabinofuranosyluracil. This product is intended for research and analytical applications. 1-beta-D-Arabinofuranosyluracil (Uracil 1-β-D-arabinofuranoside) isolated from the Caribbean sponge Tectitethya crypta, is a methoxyadenosine derivative. 1-beta-D-Arabinofuranosyluracil has demonstrated a diverse bioactivity profile including anti-inflammatory activity, analgesic and vasodilation properties . 1-beta-D-Arabinofuranosyluracil reduces a proliferation of mouse lymphoma cells .
|
-
-
- HY-30004
-
|
|
Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
|
Endogenous Metabolite
|
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
-
- HY-30004R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
Endogenous Metabolite
|
|
1-Aminocyclopropane-1-carboxylic acid (Standard) is the analytical standard of 1-Aminocyclopropane-1-carboxylic acid. This product is intended for research and analytical applications. 1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-17552S
-
|
|
|
sn-Glycero-3-phosphocholine-d9 is the deuterium labeled sn-Glycero-3-phosphocholine. sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia[1][2].
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-148254
-
|
|
|
Azide
|
|
8RK64 is a covalent UCHL1 inhibitor (IC50: 0.32 μM) . 8RK64 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-15286
-
|
|
|
Alkynes
|
|
Sodium 4-pentynoate is a alkynylacetate analogue, can be metabolically incorporated onto cellular proteins through biosynthetic mechanisms for profiling of acetylated proteins in diverse cell types . Sodium 4-pentynoate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-133870
-
|
ITalk
|
|
Alkynes
|
|
Itaconate-alkyne (ITalk) is a specific bioorthogonal probe for quantitative and site-specific chemoproteomic profiling of Itaconation in living cells. Itaconate-alkyne, a functional analogue of Itaconate, exhibits comparable antiinflammatory effect with Itaconate and enables the labeling of bona fide targets of Itaconate . Itaconate-alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-136205
-
|
Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide
|
|
Alkynes
|
|
IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection . IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling . IA-Alkyne is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-103006
-
NAI-N3
5 Publications Verification
|
|
Azide
|
|
NAI-N3 is a RNA acylation reagent that enables RNA purification. NAI-N3 is a dual-function SHAPE (selective 2-hydroxyl acylation and profiling experiment) probe (RNA structure probe and enrichment) . It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
|
-
- HY-126943
-
|
|
|
Alkynes
|
|
SAHA-BPyne is an activity-based protein profiling (ABPP) probe for detecting HDAC activity, which covalently labels the proximal proteins through a photoactivation. SAHA-BPyne inhibits HDAC activity in HeLa nuclear lysate with an IC50 of less than 5 μM .
|
-
- HY-125384
-
|
|
|
Alkynes
|
|
ARN14686 is an activity-based protein profiling (ABPP) probe. ARN14686 inhibits hNAAA with high potency (IC50=0.006 μM). ARN14686 interacts with NAAA via covalent binding to the N-terminal cysteine. ARN14686 binds only to the catalytically active form of NAAA, and may serve therefore as an efficient activity-based probe .
|
-
- HY-151872
-
|
|
|
Alkynes
|
|
HDAC-IN-48 is a potent HDAC inhibitor. HDAC-IN-48 is a hybrid molecule with great cytotoxic profile (GI50~20 nM). HDAC-IN-48 consists of harmacophores of SAHA and CETZOLE molecules. HDAC-IN-48 induces ferroptosis and inhibits HDAC proteins . HDAC-IN-48 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
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