Search Result
Results for "
monkeys
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-110252
-
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Endogenous Metabolite
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Others
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Salvinorin B is the metabolite produced by Salvia divinorum. Salvinorin B is also the main metabolite of Salvinorin A in rhesus monkey blood .
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-
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- HY-107741
-
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Opioid Receptor
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Neurological Disease
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SNC162 is a delta-opioid receptor agonist with an IC50 of 0.94 nM. SNC162 has antidepressant-like effects and produces a selective enhancement of the antinociceptive effects of fentanyl in rhesus monkeys .
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-
-
- HY-152857
-
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LY3473329
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Others
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Cardiovascular Disease
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Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a)
formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys .
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-
-
- HY-P10031A
-
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GLP Receptor
GCGR
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Metabolic Disease
|
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SAR441255 TFA is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 TFA displays high potency with balanced activation of all three target receptors. SAR441255 TFA shows positive acute glucoregulatory effectss in diabetic obese monkeys .
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-
-
- HY-111262
-
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11β-HSD
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Neurological Disease
Metabolic Disease
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ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD) .
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-
-
- HY-14568
-
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GlyT
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Neurological Disease
|
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DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey .
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-
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- HY-105034A
-
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BMY 13859-1; MJ 13859-1
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Others
|
Neurological Disease
|
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Tiospirone (MJ 13859-1) hydrochloride is an orally active antipsychotic agent that reduces or eliminates tardive dyskinesia (TD) in Cebus apella monkeys with persistent TD .
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-
-
- HY-118956
-
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ABT-431 hydrochloride; DAS-431 hydrochloride
|
Dopamine Receptor
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Neurological Disease
|
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Adrogolide hydrochloride (ABT-431 hydrochloride) is a chemically stable prodrug that can convert to the dopamine D1 receptor agonist A-86929. Adrogolide hydrochloride ameliorates the MPTP (HY-15608)-induced Parkinson's Disease in marmoset model, reduces the dyskinesias tendency. Adrogolide hydrochloride reverses Risperidone (HY-11018)-induced cognitive deficits in monkey .
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-
-
- HY-101663
-
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MK-8408
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HCV
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Infection
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Ruzasvir (MK-8408) is an orally active inhibitor for genotypic HCV nonstructural protein 5A (NS5A), which inhibits the replication of NS5A mutants GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a and GT4a with EC90 ranging from 0.003 to 0.067 nM. Ruzasvir exhibits good pharmacokinetic characters in rhesus monkey model .
|
-
-
- HY-P10031
-
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GLP Receptor
GCGR
|
Metabolic Disease
|
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SAR441255 is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 displays high potency with balanced activation of all three target receptors.?SAR441255 shows positive acute glucoregulatory effectss in diabetic obese monkeys .
|
-
-
- HY-109114A
-
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MT-7117 phosphate
|
Melanocortin Receptor
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Metabolic Disease
|
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Dersimelagon phosphate is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon phosphate shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon phosphate can be used for the research of skin pigmentation .
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-
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- HY-159099
-
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Molecular Glues
Histone Acetyltransferase
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Others
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HbF inducer 3 (Compound dWIZ-2) is an orally active molecular glue, which degrades the WIZ transcription factor (DC50=13 nM in primary human erythroid precursor cell) and induces the expression of fetal hemoglobin (HbF) (EC50=100 nM). HbF inducer 3 exhibits good pharmacokinetic characteristics in cynomolgus monkeys .
|
-
-
- HY-109114
-
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MT-7117
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Melanocortin Receptor
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Metabolic Disease
|
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Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation .
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-
-
- HY-164535
-
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AMG 133
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GLP Receptor
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Metabolic Disease
|
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Maridebart cafraglutide (AMG 133) is an antibody-peptide conjugate acting as a GLP-1 receptor agonist and an antagonist of the GIP receptor. Maridebart cafraglutide reduces body weight and improve metabolic markers in male obese mice and cynomolgus monkeys. Maridebart cafraglutide is promising for research of obesity .
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-
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- HY-145713
-
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HBV-IN-19
|
HBV
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Infection
|
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GS-8873 is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 causes neurofunctional deficits in rats and cynomolgus monkeys .
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-
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- HY-145713A
-
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HBV-IN-19 TFA
|
HBV
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Infection
|
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GS-8873 TFA is the TFA salt form of GS-8873 (HY-145713). GS-8873 TFA is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 TFA exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 TFA causes neurofunctional deficits in rats and cynomolgus monkeys .
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-
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- HY-103496
-
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GABA Receptor
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Others
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U-90042 is a gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with Ki values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent .
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-
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- HY-19145
-
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CI-992
|
Renin
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Cancer
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PD-134672 (CI-992) is a renin inhibitor containing a 2-amino-4-thiazolyl substituent. PD-134672 potently inhibits monkey renin in vitro and only weakly inhibits the related aspartic protease bovine feline hepsin D. The compound exhibits oral hypotensive activity in hyperreninemic normotensive monkeys. Based on its superior efficacy and long-lasting effects in vitro and in the normotensive macaque model, PD-134672 was selected for further evaluation in renal hypertensive monkeys.
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-
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- HY-119602
-
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CI-911
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Others
|
Neurological Disease
|
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Rolziracetam is a nootropic agent of the racetam family and improves short-term memory in rats and monkeys .
|
-
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- HY-101294
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-
-
- HY-164893
-
-
-
- HY-100254
-
-
-
- HY-111073
-
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Y101
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HBV
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Infection
Inflammation/Immunology
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Bentysrepinine (Y101) is an orally active HBV inhibitor with anti-hepatitis B virus infection activity. Bentysrepinine exhibits favorable pharmacokinetic characteristics, with absolute bioavailability of 44.9%, 43.1%, and 19.2% in rats, dogs, and monkeys, respectively, and it does not accumulate in monkeys after 90 days of oral administration. Bentysrepinine is under research in the antiviral and hepatitis fields .
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-
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- HY-137412
-
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Prostaglandin F2α 1,15-lactone
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Others
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Endocrinology
|
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PGF2α 1,15-lactone (Prostaglandin F2α 1,15-lactone) is a lipid-soluble internal ester of PGF2α. PGF2α 1,15-lactone decreases menstrual cycle lengths in non-pregnant rhesus monkeys. PGF2α 1,15-lactone terminates early pregnancy in the monkey .
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-
-
- HY-12798A
-
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AR-13324 dimesylate
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ROCK
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Others
|
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Netarsudil mesylate (AR-13324 mesylate) is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.
|
-
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- HY-101760
-
|
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RIP kinase
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Inflammation/Immunology
|
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GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .
|
-
-
- HY-112583
-
|
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Cathepsin
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Neurological Disease
|
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MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
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-
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- HY-116606
-
-
-
- HY-16308
-
|
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Phosphatase
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Metabolic Disease
|
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MB-07729 is a potent fructose 1,6-bisphosphatase (FBPase) noncompetitive inhibitor with IC50 values of 31, 121, and 189 nM for human, monkey, and rat, respectively.
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-
-
- HY-12699
-
-
-
- HY-107176A
-
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HS-25
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Others
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Metabolic Disease
|
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Hyzetimibe is a cholesterol absorption inhibitor. Hyzetimibe blocks the intestinal absorption of cholesterol and phytol. Hyzetimibe is well tolerated in animal models, with an LDmax 2000 mg/kg in rats and an LDmax 500 mg/kg in rhesus monkeys .
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-
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- HY-108446
-
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Urotensin Receptor
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Cardiovascular Disease
|
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GSK 1562590 hydrochloride is a high affinity and selective antagonist of urotensin-II receptor (UT), with pKis of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT .
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-
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- HY-122517
-
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U-24729 A
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Others
|
Others
|
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Mirincamycin (hydrochloride) (U-24729 A), a compound used to inhibit malaria, has a protective effect against the early liver stages of Plasmodium but fails to kill dormant liver stages of Plasmodium in a rhesus monkey model.
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-
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- HY-W050088
-
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HP 549
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Others
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Inflammation/Immunology
|
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Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc .
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-
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- HY-153907
-
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Drug-Linker Conjugates for ADC
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Cancer
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SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
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-
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- HY-U00369
-
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Acyltransferase
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Cardiovascular Disease
|
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FCE 28654 is an inhibitor of acylCoA: cholesterol acyltransferase (ACAT), weakly inhibiting ACAT in microsomes from rabbit aorta and intestine, and monkey liver, with IC50s of 2.55, 1.08 and 5.69 μM, respcetively.
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- HY-118185
-
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Others
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Others
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SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
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-
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- HY-34781
-
-
-
- HY-125043
-
-
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- HY-158424
-
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Others
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Cardiovascular Disease
|
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LSN3353871 is a potent inhibitor of lipoprotein(a) (Lp(a)) that can binds to Kringle IV (KIV) 8, KIV7–8 and KIV5–8, with Kd of 756 nM, 605 nM and 423 nM, respectively. LSN3353871 disrupts the formation of Lp(a) with the IC50 of 1.69 µM. LSN3353871 has oral bioactivity .
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- HY-102074
-
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Others
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Infection
|
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ERDRP-0519, an orally bioavailable small-molecule Measles virus (MeV) polymerase inhibitor, prevents measles disease in squirrel monkeys (Saimiri sciureus). ERDRP-0519 inhibits morbilliviruses with nanomolar potency. .
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-
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- HY-108620
-
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GR259653X
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys .
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-
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- HY-112209
-
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mAChR
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Neurological Disease
|
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VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
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-
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- HY-102089
-
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Dopamine Receptor
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Neurological Disease
|
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Fluoroclebopride binds reversibly to dopamine receptors. 18F labeled fluoroclebopride has been used as a probe for studying D2/D3 receptor availability via PET in various monkey models .
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-
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- HY-19513
-
-
-
- HY-19513A
-
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Thyroid Hormone Receptor
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Metabolic Disease
Endocrinology
|
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MB-07344 sodium is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM. MB-07344 sodium has additive cholesterol lowering activity in combination with Atorvastatin (HY-B0589) in rabbits, dogs and monkeys .
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-
-
- HY-B1123
-
-
-
- HY-B0770
-
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β-Arteether; (+)-Arteether; Arteether
|
CXCR
Parasite
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Infection
Cancer
|
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Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
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-
-
- HY-P99439
-
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IMA-638
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Interleukin Related
|
Inflammation/Immunology
|
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Anrukinzumab (IMA-638) is a humanized anti-IL-13 monoclonal antibody. Anrukinzumab effectively reduces lung inflammation in a cynomolgus monkey model. Anrukinzumab can be used in studies of ulcerative colitis (UC) as well as asthma .
|
-
-
- HY-10198
-
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SCH 527123; MK-7123
|
CXCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
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Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly .
|
-
- HY-145516
-
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Ro 47-8634
|
Others
|
Metabolic Disease
|
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Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.
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-
- HY-101339
-
|
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Others
|
Others
|
|
(R)-RS 56812 is a 5-HT3 receptor antagonist that enhances performance in monkeys on a delayed matching task. The (R) isomer produces more systematic improvements than the (S) isomer and has potential inhibitory effects in diseases involving cognitive decline.
|
-
- HY-101339A
-
|
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Others
|
Others
|
|
(R)-RS 56812 hydrochloride is a 5-HT3 receptor antagonist that enhances performance in monkeys on a delayed matching task. The (R) isomer produces more systematic improvements than the (S) isomer and has potential inhibitory effects in diseases involving cognitive decline.
|
-
- HY-101303
-
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Melatonin Receptor
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Others
|
|
5-MCA-NAT is a melatonin agonist that may target the melatoninMT3 receptor. 5-MCA-NAT can contract the colonic band in a concentration-dependent manner and reduce intraocular pressure (IOP) in glaucomatous monkey eyes, inhibiting the increase in IOP .
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- HY-127012
-
|
|
Others
|
Others
|
|
H-0104 dihydrochloride is a ROCK inhibitor with significant intraocular pressure (IOP)-lowering activity. H-0104 dihydrochloride effectively reduces IOP when administered to monkey eyes. There may not be a direct relationship between the Iop-lowering effect of H-0104 dihydrochloride and ROCK inhibition .
|
-
- HY-19837
-
|
|
Protease Activated Receptor (PAR)
|
Inflammation/Immunology
|
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BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
|
-
- HY-124112
-
|
|
Parasite
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Infection
|
|
PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
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-
- HY-112185
-
|
LY3502970; GLP-1 receptor agonist 1
|
GCGR
|
Metabolic Disease
|
|
Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete .
|
-
- HY-155088
-
|
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mGluR
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Metabolic Disease
|
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MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
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-
- HY-161246
-
|
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Others
|
Neurological Disease
|
|
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
|
-
- HY-112185A
-
|
LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate
|
GCGR
|
Metabolic Disease
|
|
Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete .
|
-
- HY-137043
-
|
Fluprostenol Prostaglandin E2
|
Prostaglandin Receptor
|
Endocrinology
|
|
9-Keto Travoprost is a derivative of Fluprostenol (HY-108560). 9-Keto Travoprost is an EP receptor agonist. 9-Keto Travoprost can be used in endocrine-related research .
|
-
- HY-12159
-
|
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Integrin
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Inflammation/Immunology
|
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MK-0668 is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
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-
- HY-12159A
-
|
|
Integrin
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Inflammation/Immunology
|
|
MK-0668 mesylate is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 mesylate exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
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-
- HY-W050088R
-
|
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Others
|
Inflammation/Immunology
|
|
Isoxepac (Standard) is the analytical standard of Isoxepac. This product is intended for research and analytical applications. Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc .
|
-
- HY-109042
-
|
CORT 125134
|
Glucocorticoid Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
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-
- HY-19848
-
|
LBM-642
|
PPAR
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Metabolic Disease
|
|
Cevoglitazar (LBM-642) is an orally active and highly potent PPARα and PPARγ dual agonist. Cevoglitazar can reduce food intake, body weight, and fasting plasma insulin in obese mice and cynomolgus monkeys. Cevoglitazar has the potential for diabetes and obesity-related disorders research .
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-
- HY-130249
-
|
|
GnRH Receptor
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Endocrinology
|
|
BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels .
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-
- HY-156684
-
|
|
TRP Channel
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Neurological Disease
|
|
GDC-6599 is an orally active TRPA1 inhibitor, with IC50 values of 5.3 nM in humans, 6.6 nM in rats, 9.3 nM in dogs, 7.2 nM in monkeys, and 15 nM in guinea pigs. GDC-6599 can be used in the research of neuropathic pain and respiratory diseases such as asthma and chronic cough .
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-
- HY-112144
-
|
|
HIF/HIF Prolyl-Hydroxylase
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Metabolic Disease
|
|
TP0463518 is a potent hypoxia-inducible factor prolyl hydroxylases (PHDs) inhibitor with a Ki value of 5.3 nM for human PHD2. TP0463518 also inhibits human PHD1/PHD3 with IC50s of 18 and 63 nM as well as monkey PHD2 with an IC50 value of 22 nM .
|
-
- HY-14644
-
Apilimod
Maximum Cited Publications
27 Publications Verification
STA 5326; LAM-002A free base; AIT-101
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
Cancer
|
|
Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively . Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- HY-14644A
-
|
STA 5326 mesylate; LAM-002A; AIT-101 mesylate
|
Interleukin Related
PIKfyve
|
Inflammation/Immunology
Cancer
|
|
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively . Apilimod is a potent and highly selective PIKfyve inhibitor.
|
-
- HY-121700
-
|
|
5 alpha Reductase
|
Others
|
|
L-751788 is a selective inhibitor of type I of 5α-reductase. L-751788 does not have a significant impact on the differentiation of the external genitalia in animals. When administered orally to pregnant rhesus monkeys, L-751788 (2, 10 mg/kg) did not cause abnormalities in fetal external genitalia .
|
-
- HY-P99248
-
|
Risankizumab rzaa; BI 655066
|
Interleukin Related
|
Inflammation/Immunology
|
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Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
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- HY-P0013
-
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D-21074; ORF 23541
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GnRH Receptor
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Cancer
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Antide (D-21074) is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.
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- HY-P99786
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REGN3918
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Complement System
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Metabolic Disease
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Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
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- HY-153120A
-
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PI3K
mTOR
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Cancer
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PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
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- HY-153120
-
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PI3K
mTOR
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Cancer
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PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
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- HY-149958
-
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Parasite
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Infection
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Antileishmanial agent-17 is a coumarin hybrid compound with antileishmanial effects (IC50 <0.78 μM). Antileishmanial agent-17 is safe to normal VERO cells. Antileishmanial agent-17 binds to folate pathway enzymes pteridine reductase and DHFR-TS. And Antileishmanial agent-17 shows the most potent with IC50 value of 0.40 μM against promastigote and 0.68 μM against amastigote, respectivley.
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- HY-163751
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-
- HY-109091
-
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GS-9876
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Syk
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Inflammation/Immunology
Cancer
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Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
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- HY-101930B
-
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11β-HSD
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Metabolic Disease
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(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
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- HY-A0184
-
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Ro 42-5892; Ro 42-5892/001
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Renin
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Cardiovascular Disease
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Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension .
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- HY-151500
-
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Others
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Metabolic Disease
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JBSNF-000028 is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 µM, 0.19 µM and 0.21 µM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 can be used for the research of metabolic disorders .
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- HY-151500B
-
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Others
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Metabolic Disease
|
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JBSNF-000028 hydrochloride is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 hydrochloride can be used for the research of metabolic disorders .
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- HY-117529
-
|
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Cytochrome P450
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Cancer
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BMS-351 (compound 18) is a potent, oral active, nonsteroidal CYP17A1 lyase inhibitor with the IC50 values of 19 nM and 4 nM aganist human CYP17A1 and cynomolgus monkeys CYP17A1,respectively. BMS-351 can be used for the study of castration-resistant prostate cancer .
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- HY-111156
-
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Monoamine Oxidase
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Neurological Disease
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NW-1172 (free base) (compound 22b) is a 5-HT3 receptor antagonist with performance-enhancing activity in a delayed matching task in monkeys, with the (R) isomer producing more systematic improvements than the (S) isomer, a difference paralleled by the higher affinity of the (R) enantiomer for the 5-HT3 receptor.
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- HY-119277
-
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Dopamine Receptor
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Neurological Disease
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CJB-090 dihydrochloride is a partial agonist with activity at dopamine D3 receptors. CJB-090 exhibits partial agonist characteristics in vitro. CJB-090 elicits yawning responses only in monkeys with an extensive history of cocaine use. CJB-090 reduces the reinstatement effects of cocaine in reinstatement behaviors induced by cocaine .
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- HY-113600
-
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Others
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Others
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H-0106 dihydrochloride is a ROCK inhibitor with potent intraocular pressure (IOP)-lowering activity. H-0106 dihydrochloride can effectively inhibit ROCK enzyme. H-0106 dihydrochloride demonstrated significant IOP-lowering effects in monkey eyes. Studies with H-0106 dihydrochloride suggest that there may not be a direct relationship between ROCK inhibition and IOP reduction .
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- HY-16209
-
|
BCX-1777 hydrochloride; Immucillin-H hydrochloride
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Nucleoside Antimetabolite/Analog
Apoptosis
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Cancer
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Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels .
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- HY-16210
-
|
BCX-1777; Immucillin-H
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Nucleoside Antimetabolite/Analog
Apoptosis
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Cancer
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Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels .
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- HY-P99293
-
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IDEC 114; Anti-Human CD80 Recombinant Antibody
|
CD28
|
Cancer
|
|
Galiximab (IDEC 114) is a primatized immunoglobulin G1 (IgG1) lambda monoclonal antibody directed against the CD80 antigen and blocks CD80–CD28 binding. Galiximab has variable regions are primatized (cynomologous monkeys), and the constant regions are human. Galiximab can be used in research of B-cell lymphoma .
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- HY-151500A
-
|
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Others
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Metabolic Disease
|
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JBSNF-000028 TFA is an orally active nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 0.033 μM, 0.19 μM and 0.21 μM against human NNMT (hNNMT), monkey NNMT (mkNNMT), and mouse NNMT (mNNMT), respectively. JBSNF-000028 TFA can be used for the research of metabolic disorders .
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- HY-18056
-
|
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Others
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Metabolic Disease
|
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PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
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- HY-109091B
-
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GS-9876 succinate
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Syk
|
Inflammation/Immunology
Cancer
|
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Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
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- HY-10656
-
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Urotensin Receptor
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Inflammation/Immunology
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SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
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-
- HY-109091A
-
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GS-9876 monosuccinate
|
Syk
|
Inflammation/Immunology
Cancer
|
|
Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
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- HY-P990093
-
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CM310
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Interleukin Related
|
Inflammation/Immunology
|
|
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
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- HY-123328
-
|
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Prostaglandin Receptor
|
Cardiovascular Disease
|
|
AGN 191976 is a potent and selective thromboxane A2-sensitive (TP) receptor agonist with EC50 values of 0.23 nM and 24 nM in rat aorta and human platelets, respectively. AGN 191976 has potent IOP-lowering effects in dogs and monkeys. AGN 191976 can be used to study vascular biology and the role of thromboxane A2 in vascular function .
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- HY-117090
-
|
(rac)-4,5-DHP-AMT
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Others
|
Others
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(rac)-AL-37350A ((rac)-4,5-DHP-AMT) is a 5-HT2 receptor agonist with intraocular pressure-lowering activity. (rac)-AL-37350A has high affinity and selectivity for the 5-HT2 receptor and effectively reduces intraocular pressure in conscious hypertensive cynomolgus monkeys.
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- HY-N1483A
-
|
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Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
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- HY-12811
-
|
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Sodium Channel
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Neurological Disease
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|
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect .
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- HY-P9931
-
|
CNTO 1959
|
Interleukin Related
|
Inflammation/Immunology
|
|
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research .
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- HY-107668A
-
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nAChR
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Neurological Disease
|
|
TC-1698 is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 improves memory and has neuroprotective effects. TC-1698 can be used for Alzheimer's disease research .
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- HY-107668
-
|
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nAChR
|
Neurological Disease
|
|
TC-1698 dihydrochloride is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 dihydrochloride improves memory and has neuroprotective effects. TC-1698 dihydrochloride can be used for Alzheimer's disease research .
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- HY-115864
-
|
TAK-653; NBI-1065845
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iGluR
Lipoxygenase
|
Neurological Disease
|
|
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca 2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
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- HY-P99399
-
|
RG 6100; RO7105705; MTAU-9937A
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Tau Protein
|
Neurological Disease
|
|
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
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- HY-157802
-
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Sodium Channel
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Neurological Disease
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|
LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
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- HY-P10318
-
|
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GLP Receptor
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Endocrinology
|
|
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
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- HY-157802A
-
|
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Sodium Channel
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Neurological Disease
|
|
(S)-LTGO-33 is a small molecule inhibitor of voltage-gated sodium channel NaV1.8. (S)-LTGO-33 can be used in the treatment of pain disorders .
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- HY-122229
-
|
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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 .
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-
- HY-101189
-
|
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Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
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-
- HY-112701
-
|
|
CCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer .
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- HY-101189B
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
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-
- HY-10294
-
|
SB-462795
|
Cathepsin
|
Metabolic Disease
Cancer
|
|
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
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-
- HY-145644
-
|
C-135-LS; BMS-986414
|
SARS-CoV
|
Infection
Cancer
|
|
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
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- HY-126115
-
|
15-epi Latanoprost
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Others
|
Cardiovascular Disease
Others
|
|
15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
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-
- HY-117955
-
|
WAY 141839; Co 2-6749
|
GABA Receptor
|
Neurological Disease
|
|
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics .
|
-
- HY-16785
-
|
INXN-1001; RG-115932
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys .
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-
- HY-P99737
-
|
LY3074828
|
Interleukin Related
|
Inflammation/Immunology
|
|
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkey IL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
|
-
- HY-117982
-
|
|
GnRH Receptor
ERK
|
Endocrinology
|
|
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
|
-
- HY-P99584
-
|
KD-247
|
HIV
|
Infection
|
|
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN, HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection .
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-
- HY-122542B
-
|
|
PAI-1
|
Cardiovascular Disease
|
|
PPACK TFA is a plasminogen activator (rt-PA) inhibitor. PPACK TFA can inhibit changes in fibrin degradation products, plasminogen and alpha 2-antiplasmin. PPACK TFA also inhibits the binding of rt-PA to plasma protease inhibitors .
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-
- HY-112584
-
|
6-Methoxynicotinamide
|
Others
|
Metabolic Disease
|
|
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease .
|
-
- HY-N1483
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
|
-
- HY-117637
-
|
|
Others
|
Neurological Disease
|
|
ALS-I-41 is a novel, potent and selective oxytocin receptor antagonist with the potential to modulate biological activities related to social behavior and mental disorders. ALS-I-41 is being evaluated for behavioral pharmacology experiments in non-human primates and can be administered via intranasal or intramuscular injection. The central nervous system penetration and metabolic rate of ALS-I-41 were studied by mass spectrometry analysis in cerebrospinal fluid and plasma of macaque monkeys .
|
-
- HY-16474
-
|
TAK-385
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
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-
- HY-121670
-
|
|
Others
|
Neurological Disease
|
|
Ambenoxan is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
|
-
- HY-131605
-
|
GCV-TP
|
Endogenous Metabolite
|
Cancer
|
|
Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM and has good antiviral effects against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
|
-
- HY-121670A
-
|
|
Others
|
Neurological Disease
|
|
Ambenoxan hydrochloride is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
|
-
- HY-P99030
-
|
|
EGFR
|
Cancer
|
|
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer .
|
-
- HY-P99110
-
|
SHP643; DX-2930
|
Kallikrein
|
Inflammation/Immunology
|
|
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
|
-
- HY-150080
-
|
BMS-986180
|
HIV
HIV Integrase
|
Infection
|
|
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
|
-
- HY-P99670
-
-
- HY-19109
-
|
|
Others
|
Others
|
|
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
|
-
- HY-16474S
-
|
TAK-385-d6
|
Isotope-Labeled Compounds
GnRH Receptor
|
Endocrinology
Cancer
|
|
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
|
-
- HY-16474R
-
|
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
|
-
- HY-123567
-
|
|
Others
|
Neurological Disease
|
|
LY86057 is an ergoline derivative without N1 substituents. It has higher affinity for porcine, squirrel monkey and human 5-HT2 receptors than rats and is an antagonist of 5-HT2 receptors. When studying the differences in recognition of a series of ergolines between species, LY86057 was found to be more selective for 5-HT2 receptors. Compared with LY53857, LY108742 resulted in a higher affinity for rat 5-HT2 receptors even when the N1 substituent was only methyl.
|
-
- HY-126115R
-
|
|
Others
|
Cardiovascular Disease
Others
|
|
15(S)-Latanoprost (Standard) is the analytical standard of 15(S)-Latanoprost. This product is intended for research and analytical applications. 15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
|
-
- HY-P99250
-
|
MetMAb
|
c-Met/HGFR
|
Cancer
|
|
Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
|
-
- HY-P10269
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
|
-
- HY-B1357
-
-
- HY-P99836
-
|
IBI101
|
Orexin Receptor (OX Receptor)
|
Inflammation/Immunology
Cancer
|
|
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research .
|
-
- HY-B1357R
-
|
|
Bcl-2 Family
Caspase
Apoptosis
HSV
Na+/K+ ATPase
Calcium Channel
|
Cardiovascular Disease
Cancer
|
|
Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
|
-
- HY-19306
-
|
|
Integrin
|
Cancer
|
|
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression .
|
-
- HY-U00237B
-
|
|
Others
|
Others
|
|
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
|
-
- HY-15042
-
|
|
Bradykinin Receptor
|
Metabolic Disease
|
|
MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
|
-
- HY-W127357
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Glyceryl trinonanoate is a triacylglycerol containing nonanoic acid at the sn-1, sn-2 and sn-3 positions. It has been found in Schizochytrium biomass. 1 1,2,3-Trinonanoyl-rac-glycerol increases blood levels of the ketone body D-(-)-3-hydroxybutyrate in neonatal rhesus monkeys. 2|1. Mioso, R., Toledo Marante, FJ, González, JE, et al. Schizochytrium sp. metabolite analysis. Oleaginous microbial sources of biodiesel by GC-MS. braz. J. Microbiology. 45(2), 403-409 (2014).|2. Tetrick, MA, Greer, FR and Benevenga, NJ Blood D- ( )-3-Hydroxybutyric acid concentration. Compare. medicine. 60(6), 486-490 (2010).
|
-
- HY-153360
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
MC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has high affinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells .
|
-
- HY-139124
-
|
15(R)-Carboprost; 15(R)-15-methyl PGF2α
|
Others
|
Metabolic Disease
|
|
15(R)-15-Methyl Prostaglandin F2α (15(R)-Carboprost; 15(R)-15-methyl PGF2α) is a metabolically stable analog of PGF2α. 15(R)-15-Methyl Prostaglandin F2α is an inactive, prodrug PGF agonist designed for activation by gastric acid after oral administration. Acid-catalyzed epimerization of 15(R)-15-Methyl Prostaglandin F2α converts it into the active 15(S)-isomer. The 15(S)-isomer induces luteolysis when injected in rhesus monkeys at a dose of about 12 mg/animal, while the 15(R)-isomer does not.
|
-
- HY-16622A
-
|
|
LPL Receptor
|
Others
|
|
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
|
-
- HY-14932
-
|
DB289
|
Parasite
Antibiotic
|
Infection
|
|
Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria .
|
-
- HY-12654
-
|
BAY 85-3934
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
|
-
- HY-P99263
-
|
Anti-Human selectin P Recombinant Antibody
|
P-selectin
|
Cardiovascular Disease
|
|
Inclacumab (Anti-Human selectin P Recombinant Antibody) is a human monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 μg/mL and strongly inhibits cell adhesion .
|
-
- HY-14932A
-
|
DB289 maleate
|
Parasite
Antibiotic
|
Infection
|
|
Pafuramidine (maleate) (DB289 (maleate)) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine (maleate) (DB289 (maleate)) is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria .
|
-
- HY-W747868
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia .
|
-
- HY-141899
-
|
|
mAChR
|
Neurological Disease
|
|
MK-6884 is a M4 muscarinic receptor positive allosteric modulator (PAM) with a Ki value of 0.19 nM. MK-6884 can be used for the research of the neurodegenerative diseases. MK-6884 can be conveniently radiolabeled with carbon-11 and as a positron emission tomography (PET) imaging agent .
|
-
- HY-144074
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease .
|
-
- HY-148130
-
|
RG6091; RO7248824
|
E1/E2/E3 Enzyme
|
Others
|
|
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
|
-
- HY-148130A
-
|
RG6091 sodium; RO7248824 sodium
|
E1/E2/E3 Enzyme
|
Others
|
|
Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
|
-
- HY-116889
-
|
|
Drug Metabolite
|
Others
|
|
15-keto Latanoprost is a potential metabolite of latanoprost (HY-B0577) when administered to animals. 15-keto Latanoprost is also one of the common minor impurities found in commercial preparations of the bulk drug compound. Although much less potent that the parent compound latanoprost, 15-keto latanoprost still retains the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye.1 15-keto Latanoprost is also a miotic in the normal cat eye, causing an 8 mm Hg reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type prostaglandins; for example, prostaglandin F2α will produce this degree of miosis at a dose of less than 1 μg/eye.
|
-
- HY-109968A
-
|
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-109968
-
|
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-115987
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
|
-
- HY-116161
-
|
|
Others
|
Cardiovascular Disease
Others
|
|
15(R)-17-phenyl trinor Prostaglandin F2α isopropyl ester (15(R)-17-phenyl trinor PGF2α isopropyl ester) is the latanoprost-related isomer containing both a double bond at 13,14 and an inverted (β) hydroxyl group at C-15. Similar to 15(S)-latanoprost, 15(R)-17-phenyl trinor PGF2α isopropyl ester is a potential impurity in most commercial preparations of the latanoprost bulk drug product. The IC50 values for the free acid forms of 15(S)-17-phenyl trinor PGF2α and 15(R)-17-phenyl trinor PGF2α were determined to be 0.71 nM and 30 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle.1 A 3 μg dose of 15(R)-17-phenyl trinor PGF2α caused a 1.9 mmHg reduction of IOP in normotensive cynomolgus monkeys.
|
-
- HY-153220
-
|
|
PROTACs
Btk
|
Cancer
|
|
NX-2127 (compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk) . NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells . NX-2127 is composed of PROTAC target protein ligand (red part) BTK ligand 10 (HY-168302), E3 ligase ligand (blue part) Thalidomide 5-fluoride (HY-W087383) and PROTAC Linker (black part) (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303). Among which, the conjugate of E3 ubiquitin ligase ligand + Linker compose of Thalidomide-pyrrolidine-C-piperidine-Ph-NH2 (HY-168304).
|
-
- HY-116161A
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
17-phenyl trinor PGF2α N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan trade name Bimatoprost.1 The N-ethyl amide prostaglandin prodrugs are converted to the active free acid more slowly than the analogous prostaglandin ester prodrugs such as latanoprost.2 This product is the isopropyl ester of the free acid prostaglandin which corresponds to Bimatoprost. The free acid, 17-phenyl trinor PGF2α, is a potent FP receptor agonist.3 In human and animal models of glaucoma, FP receptor agonist activity corresponds very closely with intraocular hypotensive activity. The 17-phenyl trinor PGF2α isopropyl ester derivative is examined for IOP-lowering activity during the development of latanoprost.4 At the dose of 3 μg/eye in the monkey, 17-phenyl trinor PGF2α isopropyl ester is the most potent analog tested in reducing IOP, lowering the IOP 1.3 mm Hg below the level achieved by latanoprost. However, this derivative is also significantly more irritating to the eye than latanoprost.
|
-
- HY-113778
-
|
15-keto-17-phenyl trinor PGF2α
|
Prostaglandin Receptor
|
Endocrinology
|
|
Bimatoprost is an F-series prostaglandin (PG) analog which has been approved for use as an ocular hypotensive drug.1 Oxidation of the C-15 hydroxyl group and amide hydrolysis of Bimatoprost produces 15-keto-17-phenyl trinor PGF2α. 15-keto-17-phenyl trinor PGF2α is a potential metabolite of bimatoprost when administered to animals. 15-keto PG analogs are potential minor impurities in commercial preparations of their corresponding bulk drug compounds. Although much less potent that the parent compound, 15-keto PGs still retain the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye.2 15-keto Latanoprost (15-keto-17-phenyl-13,14-dihydro trinor PGF2α isopropyl ester) is a miotic in the normal cat eye, causing an 8 mm reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type PGs; for example, PGF2α will produce this degree of miosis at a dose of less than 1 μg/eye.
|
-
- HY-159072
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Mal-Val-Ala-PAB-N(SO2Me)-Exatecan (Compound LE14) is a conjugate of an ADC toxin Exatecan (HY-13631) and a linker Mal-Val-Ala-PAB-N(SO2Me). Mal-Val-Ala-PAB-N(SO2Me)-Exatecan can be used for synthesis of ADC FZ-AD005. FZ-AD005 is a delta-like ligand 3 (DLL3, KD=58.3 pM) targeting ADC, that exhibits antitumor efficacy against SCLC cancer .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-W127357
-
|
|
Drug Delivery
|
|
Glyceryl trinonanoate is a triacylglycerol containing nonanoic acid at the sn-1, sn-2 and sn-3 positions. It has been found in Schizochytrium biomass. 1 1,2,3-Trinonanoyl-rac-glycerol increases blood levels of the ketone body D-(-)-3-hydroxybutyrate in neonatal rhesus monkeys. 2|1. Mioso, R., Toledo Marante, FJ, González, JE, et al. Schizochytrium sp. metabolite analysis. Oleaginous microbial sources of biodiesel by GC-MS. braz. J. Microbiology. 45(2), 403-409 (2014).|2. Tetrick, MA, Greer, FR and Benevenga, NJ Blood D- ( )-3-Hydroxybutyric acid concentration. Compare. medicine. 60(6), 486-490 (2010).
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10031A
-
|
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
SAR441255 TFA is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 TFA displays high potency with balanced activation of all three target receptors. SAR441255 TFA shows positive acute glucoregulatory effectss in diabetic obese monkeys .
|
-
- HY-12523
-
|
|
Peptides
|
Others
|
|
Peptide M is a synthetic amino acid (18 amino acids in length which correspond to the amino acid positions 303-322 of bovine S-antigen: DTNLASSTIIKEGIDKTV), is capable of inducing experimental autoimmune uveitis in monkeys and Hartley guinea pigs as well as Lewis rats .
|
-
- HY-P0013
-
|
D-21074; ORF 23541
|
GnRH Receptor
|
Cancer
|
|
Antide (D-21074) is a potent LHRH antagonist. Antide also can be used for the research of prostatic cancer.
|
-
- HY-P5647
-
|
|
Peptides
|
Infection
|
|
PhD1 is an antimicrobial peptide derived from monkey white blood cells. PhD1 has activity against bacteria and fungus Candida albicans .
|
-
- HY-P5648
-
|
|
Peptides
|
Infection
|
|
PhD2 is an antimicrobial peptide derived from monkey white blood cells. PhD2 has activity against bacteria and fungus Candida albicans .
|
-
- HY-P5649
-
|
|
Peptides
|
Infection
|
|
PhD3 is an antimicrobial peptide derived from monkey white blood cells. PhD3 has activity against bacteria and fungus Candida albicans .
|
-
- HY-P5651
-
|
|
Peptides
|
Infection
|
|
PhD4 is an antimicrobial peptide derived from monkey white blood cells. PhD4 has activity against bacteria and fungus Candida albicans .
|
-
- HY-P10031
-
|
|
GLP Receptor
GCGR
|
Metabolic Disease
|
|
SAR441255 is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 displays high potency with balanced activation of all three target receptors.?SAR441255 shows positive acute glucoregulatory effectss in diabetic obese monkeys .
|
-
- HY-P5208
-
|
|
Peptides
|
Cancer
|
|
CBLB 612 is an anti-radiation agent. CBLB 612 can be used in the propagation of mouse and monkey moderate stimulation hematopoietic stem cell (HSC), and lure that they are passed to peripheral blood from bone marrow into. CBLB 612 is an important auxiliary agent for cancer .
|
-
- HY-P5049
-
|
|
Peptides
|
Others
|
|
β-MSH (monkey) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
|
-
- HY-P10318
-
|
|
GLP Receptor
|
Endocrinology
|
|
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
|
-
- HY-P5448
-
|
|
Peptides
|
Others
|
|
MOG (92–106), mouse, rat is a biological active peptide. (This is amino acids 92 to 106 fragment of the myelin oligodendrocyte glycoprotein (MOG) from mouse/rat. Mice with MOG (92–106)-induced experimental autoimmune encephalomyelitis develop extensive B cell reactivity against secondary myelin antigens. Despite the fact that this MOG peptide induces only weak T cell responses, MOG-induced autoimmunity is very severe. This peptide is encephalitogenic in SJL mice, DA rats, and rhesus monkeys.)
|
-
- HY-P10269
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990189
-
|
|
Inhibitory Antibodies
|
Others
|
|
Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) is a mouse-derived IgG2a, κ type antibody inhibitor, targeting to monkey/human MHC class II.
|
-
- HY-P990133
-
|
|
Inhibitory Antibodies
|
Others
|
|
Anti-Monkey/Human CD40L/CD154 Antibody (5C8) is a mouse-derived IgG2a type antibody inhibitor, targeting to monkey/human CD40L/CD154.
|
-
- HY-P990107
-
-
- HY-P99439
-
|
IMA-638
|
Interleukin Related
|
Inflammation/Immunology
|
|
Anrukinzumab (IMA-638) is a humanized anti-IL-13 monoclonal antibody. Anrukinzumab effectively reduces lung inflammation in a cynomolgus monkey model. Anrukinzumab can be used in studies of ulcerative colitis (UC) as well as asthma .
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- HY-P99248
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Risankizumab rzaa; BI 655066
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Interleukin Related
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Inflammation/Immunology
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Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
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- HY-P99786
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REGN3918
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Complement System
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Metabolic Disease
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Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
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- HY-P990136
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Inhibitory Antibodies
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Others
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Anti-Monkey/Human CD28 Antibody (CD28.2) is a mouse-derived IgG1, κ type antibody inhibitor, targeting to monkey/human CD28.
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- HY-P990138
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Inhibitory Antibodies
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Others
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Anti-Monkey/Human CD20 Antibody (2H7) is a mouse-derived IgG2b, κ type antibody inhibitor, targeting to monkey/human CD20.
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- HY-P990196
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Inhibitory Antibodies
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Others
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Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is a mouse-derived IgG2a, κ type antibody inhibitor, targeting to monkey/human MDR-1/CD243.
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- HY-P990236
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Inhibitory Antibodies
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Others
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Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) is a Armenian hamster-derived IgG type antibody inhibitor, targeting to mouse/rat/monkey/human ICOS/CD278.
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- HY-P99293
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IDEC 114; Anti-Human CD80 Recombinant Antibody
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CD28
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Cancer
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Galiximab (IDEC 114) is a primatized immunoglobulin G1 (IgG1) lambda monoclonal antibody directed against the CD80 antigen and blocks CD80–CD28 binding. Galiximab has variable regions are primatized (cynomologous monkeys), and the constant regions are human. Galiximab can be used in research of B-cell lymphoma .
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- HY-P990093
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CM310
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Interleukin Related
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Inflammation/Immunology
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Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
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- HY-P9931
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CNTO 1959
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Interleukin Related
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Inflammation/Immunology
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Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research .
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- HY-P99399
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RG 6100; RO7105705; MTAU-9937A
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Tau Protein
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Neurological Disease
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Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
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- HY-145644
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C-135-LS; BMS-986414
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SARS-CoV
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Infection
Cancer
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Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
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- HY-P99737
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LY3074828
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Interleukin Related
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Inflammation/Immunology
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Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkey IL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
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- HY-P99414
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- HY-P99584
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KD-247
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HIV
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Infection
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Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN, HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection .
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- HY-P99030
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EGFR
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Cancer
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Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer .
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- HY-P99110
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SHP643; DX-2930
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Kallikrein
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Inflammation/Immunology
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Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
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- HY-P99670
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-
- HY-P99250
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MetMAb
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c-Met/HGFR
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Cancer
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Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
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- HY-P99836
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IBI101
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Orexin Receptor (OX Receptor)
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Inflammation/Immunology
Cancer
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Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research .
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- HY-P99263
-
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Anti-Human selectin P Recombinant Antibody
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P-selectin
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Cardiovascular Disease
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Inclacumab (Anti-Human selectin P Recombinant Antibody) is a human monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 μg/mL and strongly inhibits cell adhesion .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-16474S
-
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Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
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| Cat. No. |
Product Name |
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Classification |
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- HY-129737
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Azide
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A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
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| Cat. No. |
Product Name |
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Classification |
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- HY-148130A
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RG6091 sodium; RO7248824 sodium
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Antisense Oligonucleotides
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Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
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- HY-148130
-
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RG6091; RO7248824
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|
Antisense Oligonucleotides
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Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
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