Search Result
Results for "
(R)-AS-1
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
15
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-14307A
-
|
Drug Isomer
|
Cancer
|
(R)-Necrocide 1 (compound (R)-38) a potent anticancer agent. (R)-Necrocide 1 has antiproliferative activity [1].
|
-
-
- HY-116463D
-
|
Sigma Receptor
|
Neurological Disease
|
(Rac)-E1R (Compound 2) is the racemate of E1R. (Rac)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) used for the research of cognition/memory disorders [1].
|
-
-
- HY-112484
-
|
Organoid
|
Cancer
|
RS-246204 is a R-spondin-1 substitute compound that is able initiate small intestinal organoids without the use of the R-spondin-1 protein.
|
-
-
- HY-168773
-
|
EAAT
|
Neurological Disease
|
(R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. (R)-AS-1 (at doses of 60 and 90 mg/kg) increases spontaneous locomotor activity in mice. Additionally, it demonstrates anticonvulsant activity in mouse models of seizures induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electrical stimuli (32 or 44 mA), with ED50s of 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively. (R)-AS-1 can be used in neurological disease research [1].
|
-
-
- HY-146410
-
|
Angiotensin Receptor
|
Others
|
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes [1].
|
-
-
- HY-149481
-
|
Dopamine Receptor
|
Neurological Disease
|
D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders [1].
|
-
-
- HY-170789
-
|
Histamine Receptor
|
Neurological Disease
|
H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). H1R ligand-1 can be used as a scaffold to design and synthesize a set of derivatives to explore H1R binding kinetics [1].
|
-
-
- HY-144033
-
|
GCGR
|
Metabolic Disease
|
GLP-1R agonist 1 is a potent agonist of GLP-1R. GLP-1R agonist 1 is a thickened imidazole derivative compound. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 1 has the potential for the research of diabetes (extracted from patent WO2021197464A1, compound 4) [1].
|
-
-
- HY-156017
-
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
5-HT6R antagonist 1 (Comopund 8) is a 5-HT6R antagonist (Ki: 5 nM). 5-HT6R antagonist 1 inhibits platelet aggregation. 5-HT6R antagonist 1 has excellent metabolic stability. 5-HT6R antagonist 1 reverses MK-801 (HY-15084B)-induced memory impairments in rats. 5-HT6R antagonist 1 can be used for Alzheimer's disease (AD) research [1].
|
-
-
- HY-143425A
-
|
MALT1
|
Cancer
|
(R)-MALT1-IN-7 (compound 142a) is a potent MALT1 protease inhibitor. (R)-MALT1-IN-7 has the potential for cancer research [1].
|
-
-
- HY-13030A
-
|
Epigenetic Reader Domain
|
Cancer
|
(R)-(-)-JQ1 Enantiomer is the stereoisomer of (+)-JQ1. (+)-JQ1 potently decreases expression of both BRD4 target genes, whereas (R)-(-)-JQ1 Enantiomer has no effect.
|
-
-
- HY-168364
-
|
Wnt
β-catenin
Drug Derivative
|
Neurological Disease
|
1(R),2(S)-epoxy Cannabidiol (Compound 2a) is a structural analogue of phytocannabinoidsphytocannabinoids. 1(R),2(S)-epoxy Cannabidiol exhibits potent inhibitory activity against Wnt/β-catenin pathway. 1(R),2(S)-epoxy Cannabidiol is promising for research of neuroprotective agents [1].
|
-
-
- HY-149941
-
|
Neurotensin Receptor
|
Neurological Disease
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent [1].
|
-
-
- HY-149014
-
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
OX2R-IN-1 (compound 15) is a low cytotoxicity profile OX2R-IN-1 antagonist (a potential OX2R binder) with an IC50 value of 484 μM. OX2R-IN-1 (compound 15) can cross the BBB into the brain with a short half-life [1].
|
-
-
- HY-146431
-
|
Angiotensin Receptor
|
Others
|
AT1R antagonist 1 (compound 10) is a potent AT1R selective ligand. AT1R antagonist 1 exhibits a fair AT1R affinity, with a Ki of 8.5 nM [1].
|
-
-
- HY-147532
-
|
Cannabinoid Receptor
|
Cancer
|
CB2R probe 1 is a safe and green CB2R (cannabinoid 2 receptor) fluorescent probe with an Ki of 130 nM. CB2R probe 1 shows low cytotoxicity in cancer cells [1].
|
-
-
- HY-159731
-
-
-
- HY-134968A
-
|
Tau Protein
|
Neurological Disease
|
(R)-TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor. (R)-TTBK1-IN-1 is an enantiomer of TTBK1-IN-1 (HY-134968). (R)-TTBK1-IN-1 can be used in the research of alzheimer’s disease and related tauopathies [1]. (R)-TTBK1-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-161405
-
|
Neuropeptide FF Receptor
Opioid Receptor
|
Neurological Disease
|
NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively .
|
-
-
- HY-145837
-
|
Neuropeptide Y Receptor
|
Cancer
|
Y1R probe-1 (Compound 39) is a high-affinity fluorescence probe for the Neuropeptide Y Y1 Receptor. Y1R probe-1 has the potential for the research of cancer disease [1].
|
-
-
- HY-145905
-
|
Dopamine Receptor
|
Neurological Disease
|
D4R antagonist-1 is a potent and selective D4R antagonist with an IC50 of 6.87 µM. D4R antagonist-1 has the potential for the research of Parkinson’s disease [1].
|
-
-
- HY-N3461
-
|
Others
|
Others
|
Isorauhimbine is an alkaloid, can be isolated from R. serpentina .
|
-
-
- HY-N7774
-
|
Others
|
Others
|
Echinatine N-oxide is a pyrrolizidine alkaloid found in R. graeca .
|
-
-
- HY-158100
-
-
-
- HY-P4745
-
|
MCHR1 (GPR24)
|
Metabolic Disease
|
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research [1].
|
-
-
- HY-152576
-
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role [1].
|
-
-
- HY-15609
-
-
-
- HY-147557
-
|
PACAP Receptor
|
Neurological Disease
|
PAC1R antagonist 1 (compound 3d) is a potent and orally active antagonist of PAC1 receptor. PAC1R antagonist 1 can inhibit pituitary adenylate cyclase-activating polypeptide (PACAP)- and nerve injury-induced allodynia [1].
|
-
-
- HY-159835
-
-
-
- HY-142165S
-
-
-
- HY-131578
-
-
-
- HY-151146
-
|
Thrombin
|
Cardiovascular Disease
|
(1R,3S)-THCCA-Asn (4j) is a selective thrombin inhibitor with the IC50 value in the range of 0.07 to 0.14 μM. ((1R,3S)-THCCA-Asn has antithrombotic activity [1].
|
-
-
- HY-168098
-
|
P2Y Receptor
|
Inflammation/Immunology
|
P2Y6R antagonist 1 (compound 5ab) is a selective, orally active P2Y6R antagonist with an IC50 value of 19.6 nM. P2Y6R antagonist 1 has anti-inflammatory activity [1].
|
-
-
- HY-14519CS
-
-
-
- HY-B0573CS
-
-
-
- HY-14948S1
-
-
-
- HY-133171AS3
-
-
-
- HY-125545
-
|
Others
|
Others
|
Cynanester A is a active product that can be isolated from Cynanchum chinense R. Br. .
|
-
-
- HY-143777S
-
-
-
- HY-B0317DS
-
-
-
- HY-P990844
-
|
Complement System
|
Others
|
Anti-GC1q R/C1QBP Antibody (60.11) is a kind of mouse IgG1, κ chimeric antibody, targeting to human GC1q R/C1QBP. The recommend isotype control of Anti-GC1q R/C1QBP Antibody (60.11): Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
-
- HY-149358
-
|
Neurokinin Receptor
|
Endocrinology
|
NK3R-IN-1 (compound 16x), a imidazolepiperazine derivative, is an orally active Neurokinin Receptor NK3R inhibitor. NK3R-IN-1 decreases blood luteinizing hormone levels in ovariectomy (OVX) model [1].
|
-
-
- HY-149715
-
|
ICMT
|
Cancer
|
R1-11 is an indole ICMT inhibitor with an IC50 of 0.6 μM and has anticancer activity. R1-11 inhibits MDA-MB231 and PC3 cells with IC50s of 2.2 μM and 2.0 μM, respectively [1].
|
-
-
- HY-149803
-
|
Sigma Receptor
|
Neurological Disease
|
S1R agonist 1 (Compound 6b) is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity [1].
|
-
-
- HY-153918
-
|
Androgen Receptor
|
Cancer
|
(R)-SKBG-1 is an RNA-binding protein NONO inhibitor. (R)-SKBG-1 suppresses androgen receptor expression with IC50s of 3.1 μM and 5.5 μM against AR-FL mRNA and AR-V7 mRNA, respectively [1].
|
-
-
- HY-149803A
-
|
Sigma Receptor
|
Neurological Disease
|
S1R agonist 1 (Compound 6b) hydrochloride is a selective S1R agonist with Kis of 0.93 nM and 72 nM for S1R and S2R, respectively. S1R agonist 1 hydrochloride exhibits neuroprotection against ROS and NMDA-induced neurotoxicity [1].
|
-
-
- HY-115774
-
-
-
- HY-P3359
-
-
-
- HY-121703
-
|
Others
|
Others
|
Rutacridone is an alkaloid that can be cultured from Ruta graveolens L. strain R-19 .
|
-
-
- HY-N10644
-
|
Others
|
Others
|
Complanatin is an acylated flavonol glycoside, it can be isolated from Astragalus complanatus R. Br .
|
-
- HY-W067673
-
|
Bacterial
|
Infection
|
4-Methoxycoumarin (Compound 6) shows antibacterial activity of against R. solanacearum .
|
-
- HY-N3591
-
|
Others
|
Others
|
cis-Methylisoeugenol (compound 10) can be isolated from the MeOH extract of R. fasciculatum .
|
-
- HY-169116
-
|
Dopamine Receptor
|
Neurological Disease
|
D5R agonist 1 (Compound 5j) is a selective, orally active and BBB penetrable D5R partial agonist (EC50: 269.7 nM). D5R agonist 1 enhances the cognition in the Scopolamine (HY-N0296)-induced amnesia model [1].
|
-
- HY-151523
-
|
Ras
|
Cancer
|
KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research [1].
|
-
- HY-149337
-
|
Dopamine Receptor
|
Neurological Disease
|
D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling [1].
|
-
- HY-114862
-
13,14-dihydro-15(R)-PGE1
|
Endogenous Metabolite
|
Others
|
13,14-dihydro-15(R)-Prostaglandin E1 (13,14-dihydro-15(R)- PGE1) is an analog of 13,14-dihydro- PGE1 which has the hydroxyl group at C-15 in the unnatural R configuration .
|
-
- HY-118926
-
|
Parasite
|
Others
|
Bioresmethrin is an insecticide that protects grain. Bioresmethrin against malathion-resistant and susceptible strains R. dominica .
|
-
- HY-145595A
-
|
Ferroptosis
|
Others
|
(1R,3R)-Ferroptosis inducer-1 is an isomer of Ferroptosis inducer-1 (HY-145595). (1R,3R)-Ferroptosis inducer-1 (compound BX-3a) is a Ferroptosis inducer with antitumor potential [1].
|
-
- HY-143422A
-
|
MALT1
|
Cancer
|
(R)-MALT1-IN-3 (compound 121) is a potent MALT1 protease inhibitor with an IC50 of 20 nM. (R)-MALT1-IN-3 has IC50 of 60 nM, 40 nM for human IL6/IL10 in OCI-LY3 cells, respectively [1].
|
-
- HY-15015
-
Oxytocin receptor antagonist 1
|
Oxytocin Receptor
|
Endocrinology
|
OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.
|
-
- HY-170006S
-
-
- HY-101774
-
|
c-Fms
|
Cancer
|
CSF1R-IN-1 is a CSF1R inhibitor with an with an IC50 of 0.5 nM.
|
-
- HY-111501
-
|
Histamine Receptor
|
Inflammation/Immunology
Endocrinology
|
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R [1].
|
-
- HY-W004758
-
|
Drug Intermediate
|
Others
|
1-(4-Chlorophenyl)piperazine is a chemical intermediate, and can be used for synthesis of D2R ligand .
|
-
- HY-126719
-
|
Drug Derivative
|
Neurological Disease
|
R-1 Methanandamide Phosphate is a water-soluble prodrug analog of arachidonylethanolamide (AEA). AEA is an endogenous cannabinoid compound [1].
|
-
- HY-161382
-
|
Neuropeptide FF Receptor
|
Neurological Disease
|
NPFF2-R ligand 1 (Compound 16a) is a NPFF2-R ligand, with Kis of 228 and 27 nM for NPFF1-R and NPFF2-R respectively. NPFF2-R ligand 1 can be used for research related with central nervous system [1].
|
-
- HY-115428
-
|
Cannabinoid Receptor
|
Others
|
(R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide (Compound 19) is the analogue of endogenous cannabinoid receptor ligand Anandamide (HY-10863). (R)-(+)-Linoleyl-1'-Hydroxy-2'-Propylamide shows weak binding affinity for CB1 and CB2 with Kis of both 21 μM [1].
|
-
- HY-151247
-
|
GnRH Receptor
|
Cancer
|
GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing [1].
|
-
- HY-162998
-
-
- HY-100328
-
-
- HY-W063149
-
|
Drug Intermediate
|
Others
|
(1S,3R)-3-Aminocyclopentanol is a synthetic intermediate useful for pharmaceutical synthesis.
|
-
- HY-113636
-
-
- HY-155336
-
-
- HY-P1726
-
-
- HY-158187S
-
R-(+)-Cifenline-d4; R-(+)-Ro 22-7796-d4
|
Isotope-Labeled Compounds
|
Others
|
R-(+)-Cibenzoline-d4 (R-(+)-Cifenline-d4) is deuterium labeled R-(+)-Cibenzoline ((R-(+)-Cifenline) .
|
-
- HY-124534
-
-
- HY-116463C
-
|
Sigma Receptor
|
Neurological Disease
|
(2R,3R)-E1R (Compound 2b) is an enantiomer of E1R. (2R,3R)-E1R is a sigma-1 receptor positive allosteric modulator (Sig1R PAM) for the treatment of cognition/memory disorders [1].
|
-
- HY-161727
-
|
P2Y Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis [1].
|
-
- HY-159941
-
|
Tau Protein
α-synuclein
Amyloid-β
|
Neurological Disease
|
tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice [1].
|
-
- HY-153277
-
-
- HY-W755107
-
|
Drug Intermediate
|
Others
|
(1S,3R)-3-Hydroxycyclopentane carboxylic acid methyl ester is a synthetic intermediate useful for pharmaceutical synthesis.
|
-
- HY-W034099
-
|
Drug Intermediate
|
Others
|
(1R,3R)-3-Hydroxycyclopentane carboxylic acid methyl ester is a synthetic intermediate useful for pharmaceutical synthesis.
|
-
- HY-128523
-
-
- HY-128523A
-
|
Cathepsin
|
Inflammation/Immunology
|
Kgp-IN-1 hydrochloride is an arginine-specific gingipain (Rgp) inhibitor extracted from patent WO2017201322A1, compound 13-R .
|
-
- HY-170687
-
-
- HY-12405
-
-
- HY-P99004
-
|
Melanocortin Receptor
|
Inflammation/Immunology
|
(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family [1].
|
-
- HY-153816A
-
-
- HY-W396889
-
-
- HY-107382
-
-
- HY-149336
-
-
- HY-155481A
-
|
Cannabinoid Receptor
|
Others
|
CB2 receptor antagonist 4 (compound (R)-1) is a CB2R-selective inverse agonist with a Kd value of 39 nM [1].
|
-
- HY-107382A
-
-
- HY-N10936
-
|
Others
|
Others
|
Denudaquinol is a phenolic derivative. Denudaquinol can be isolated from M. denudata. Denudaquinol has cytotoxicity against the SFME and r/mHMSFME-1 cell lines [1].
|
-
- HY-168571
-
-
- HY-162254
-
|
EGFR
Ack1
|
Cancer
|
EGFR T790M/L858R/ACK1-IN-1 is a dual inhibitor of EGFR T790M/L858R and ACK1. IC50 values are 23 and 263 nM, respectively. EGFR T790M/L858R/ACK1-IN-1 can inhibit cell proliferation and has antitumor activity [1].
|
-
- HY-162062
-
|
EGFR
|
Cancer
|
EGFR WT/T790M/L858R-IN-1 (compound 10d) is a potent EGFR inhibitor, with IC50s of 0.097, 0.280, and 0.051?μM for EGFR WT, EGFR T790M, and EGFR L858R, respectively. EGFR WT/T790M/L858R-IN-1 can be used for the research of cancer [1].
|
-
- HY-163229
-
|
Ligands for E3 Ligase
Autophagy
|
Cancer
|
(1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-402309
-
|
IGF-1R
EGFR
Trk Receptor
|
Neurological Disease
|
IGF-1R modulator 1 (Example 5) is an IGF-1R modulator, with EC50s of 0.29 μM (FGFR1), 0.25 μM (IGF1R), 0.34 μM (TrkA), 0.39 μM (TrkB). IGF-1R modulator 1 can be used for research of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease [1].
|
-
- HY-10013B
-
MK0364 (1R,2R)stereoisomer
|
Cannabinoid Receptor
|
Others
|
Taranabant (1R,2R)stereoisomer is the R-enantiomer of Taranabant. Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist.
|
-
- HY-145234
-
-
- HY-112219A
-
-
- HY-136072A
-
(1R,2S)-QPX7728 disodium
|
Drug Derivative
|
Others
|
(1R,2S)-Xeruborbactam ((1R,2S)-QPX7728) disodium is a boronic acid derivative [1].
|
-
- HY-133080
-
|
GnRH Receptor
|
Cancer
|
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively .
|
-
- HY-P4043
-
|
HBV
|
Infection
Inflammation/Immunology
|
Hepatitis b virus pre-s region (120-145) is a preS2 peptide that inhibits the binding of single-chain Fv fragment (scFv) or IgG to r-HBsAg .
|
-
- HY-W045221
-
-
- HY-B0462C
-
|
Histamine Receptor
|
Inflammation/Immunology
|
(R)-Azelastine hydrochloride, an antihistamine, has been demonstrated to down-regulate the levels of H1R, M1R, and M3R, while also inhibiting the proliferation of HNEpC.
|
-
- HY-139677
-
-
- HY-P990871
-
|
Integrin
|
Others
|
Anti-CD11a/LFA-1α Antibody (R7-1) is a kind of mouse IgG1 chimeric antibody, targeting to human CD11a/LFA-1α. The recommend isotype control of Anti-CD11a/LFA-1α Antibody (R7-1): Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
- HY-170950
-
|
P2Y Receptor
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
P2Y14 antagonist 1 (compound 45) is a high selective and orally active P2Y14R antagonist with an IC50 of 0.70 nM. P2Y14R antagonist 1 demonstrates significant anti-inflammatory efficacy, effectively mitigating the pulmonary infiltration of immune cells and inflammatory response through suppressing the NLRP3 signaling pathway. P2Y14R antagonist 1 has the potential for the research of acute lung injury [1].
|
-
- HY-112219
-
-
- HY-P1504
-
-
- HY-168348
-
|
PROTAC Linkers
|
Others
|
(R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline is a linker for NX-2127 (HY-153220A) [1].
|
-
- HY-W890392
-
|
PROTAC Linkers
|
Cancer
|
(1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate is a PROTAC linker used in the synthesis of SMD-1087 (HY-170828) [1].
|
-
- HY-I0718
-
|
Biochemical Assay Reagents
|
Others
|
(R)-(-)-1,1'-Binaphthyl-2,2'-diyl Hydrogenphosphate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-P990084
-
|
IGF-1R
|
Cancer
|
Veligrotug is an IgG1-kappa, anti-IGF1R (insulin-like growth factor 1 receptor, CD221) chimeric monoclonal antibody [1].
|
-
- HY-103330
-
-
- HY-U00396
-
-
- HY-N12306
-
|
Others
|
Others
|
5,7,3',4'-Tetrahydroxy-6-methoxyflavanone-7-glucoside (compound4) can be isolated from the Salvia plebeia R.Br .
|
-
- HY-139677A
-
-
- HY-162694
-
|
Ferroptosis
|
Neurological Disease
|
Ferroptosis-IN-10 (compound D1) is an inhibitor of ferroptosis with an IC50 value of 22 nM. Ferroptosis-IN-10 has neuroprotection activity in an oxygen-glucose deprivation/reoxygenation (OGD/R) model .
|
-
- HY-P1504A
-
-
- HY-P4386
-
|
GLP Receptor
|
Metabolic Disease
|
(Asp28)-Exenatide is a degradation product of exenatide (HY-13443). (Asp28)-Exenatide can be used as a GLP-1R agonist .
|
-
- HY-108494
-
|
LPL Receptor
|
Cardiovascular Disease
|
CYM50260 is a potent and exquisitely selective sphingosine-1-phosphate 4 receptor (S1P4-R) agonist with an EC50 of 45 nM. CYM50260 displays no activity against S1P1-R, S1P2-R, S1P3-R and S1P5-R [1].
|
-
- HY-19870
-
-
- HY-P99712
-
hz208F2-4
|
IGF-1R
ADC Antibody
|
Cancer
|
Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody that can be used for the synthesis of antibody–agent conjugates (ADC) [1].
|
-
- HY-116146
-
-
- HY-N3199
-
|
Bacterial
|
Infection
|
Neorauflavene is a phenolic neorautanenia isoflavanoid isolated from Neorautanenia edulis. Neorauflavene shows antibacterial activities against E. faecalis, S. suis, S. agalactiae, P. aeruginosa, B. subtilis, and R. anatipestifer .
|
-
- HY-19870A
-
-
- HY-124863A
-
|
SphK
|
Inflammation/Immunology
|
(R)-AAL is an immunomodulator. (R)-AAL decreases circulating T lymphocytes in rats, with an ID50 value of 0.009 mg/kg. (R)-AAL is a substrate of sphingosine kinase (SphK), which catalyzes the phosphorylation of (R)-AAL .
|
-
- HY-161418
-
|
Adenosine Receptor
|
Neurological Disease
|
1-NBX is a potent and selective A1R ligand. 1-NBX exhibits significantly improved A1R affinity with with a Ki of 2.6 nM and lower affinity for the A2A receptor with a Ki of 164 nM [1].
|
-
- HY-P10474
-
|
Drug Isomer
|
Others
|
RYTVELA is a deriviative of the peptide antagonist of interleukin-1 receptor 1 (IL-1R1) d-(RYTVELA) (HY-P10353) that contains all L-amino acids [1].
|
-
- HY-100013A1
-
|
GPR88
|
Neurological Disease
|
(1R,2R)-2-PCCA hydrochloride is a diastereomer of 2-PCCA, and acts as a potent GPR88 receptor agonist, with an EC50 of 3 nM in cell-free assay, and 603 nM in cell assay.
|
-
- HY-P10827
-
|
Complement System
|
Inflammation/Immunology
|
PIC1 PA, a 15 amino-acid peptide, is a potent PIC1 analog that inhibits classical pathway mediated complement activation. PIC1 PA functionally disrupts the C1s-C1r-C1r-C1s/MASPs interaction with collagen-like region (CLR) of C1q/MBL, respectively. PIC1 PA specifically binds to the CLR of C1q and bounds to purified C1q with a mean equilibrium dissociation constant (KD) of 33.3 nM [1].
|
-
- HY-Z12728
-
|
Histamine Receptor
|
Inflammation/Immunology
|
(R)-Azelastine is an antihistamine compound with antiallergic activity. (R)-Azelastine can downregulate the levels of H1R, M1R, and M3R. (R)-Azelastine has also been shown to inhibit the proliferation of HNEpC [1].
|
-
- HY-116819A
-
|
GCGR
|
Metabolic Disease
|
VU0453379 hydrochloride is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM [1].
|
-
- HY-P990777
-
-
- HY-101116
-
|
GCGR
|
Metabolic Disease
|
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM [1].
|
-
- HY-116819
-
|
GCGR
|
Metabolic Disease
|
VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM [1].
|
-
- HY-N10562
-
|
P-glycoprotein
|
Cancer
|
Mutabilol (compound 1) is a potent p-glycoprotein (P-gp) regulator. Mutabilol is a nature product could be isolated from Plectranthus mutabilis leaves. Mutabilol increases the P-gp expression in NCI-H460/R cells .
|
-
- HY-P4385
-
|
PTHR
|
Metabolic Disease
|
(Asn10,Leu11,D-Trp12)-pTH-Related Protein (7-34) amide (human, mouse, rat) is a potent PTH-1R antagonist .
|
-
- HY-156239
-
-
- HY-125527AS
-
17(R)-RvD1-d5; AT-RvD1-d5
|
Isotope-Labeled Compounds
TRP Channel
|
Inflammation/Immunology
|
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells [1]. 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
|
-
- HY-W103964
-
|
HCV
|
Infection
|
HCV-IN-47 (Compound (R)-1) shows anti-hepatitis C virus (HCV) activity with an EC50 value of 0.032 μM. HCV-IN-47 is promising for research of hepatitis C virus pathogenesis, and host-virus interaction [1].
|
-
- HY-B0462D
-
(+)-AzelAStine
|
Histamine Receptor
|
Inflammation/Immunology
|
(S)-Azelastine ((+)-Azelastine) is an antihistamine with antiallergic and antiasthmatic activity. (S)-Azelastine has been shown to downregulate H1R, M1R, and M3R levels. (S)-Azelastine also has the property of inhibiting HNEpC proliferation [1].
|
-
- HY-157391
-
-
- HY-W006202
-
(1S,3R)-3-[(tert-Butoxycarbonyl)amino]cyclopentanecarboxylic acid
|
Drug Intermediate
|
Others
|
BOC-(1S,3R)-3-aminocyclopentanecarboxylic acid ((1S,3R)-3-[(tert-Butoxycarbonyl)amino]cyclopentanecarboxylic acid) is a synthetic intermediate useful for pharmaceutical synthesis.
|
-
- HY-147625
-
|
GLP Receptor
|
Metabolic Disease
|
GLP-1R agonist 12 (Compound 123) is an agonist of glucagon-like peptide-1 receptors (GLP-1R). GLP-1R agonist 12 can be used for diabetes research [1].
|
-
- HY-151107
-
|
Cannabinoid Receptor
|
Neurological Disease
|
CBR Agonist-2 is a CB1 agonist (CB1R; CB1 ligand) with an EC50 and a Ki of 960 nM and 970 nM, respectively. CBR Agonist-2 is a promising tool for investigating the involvement of hCB1R in disorders associated with the endocannabinoid system [1].
|
-
- HY-20074
-
(1S,2S,3R,5S)-(+)-Pinanediol
|
Biochemical Assay Reagents
|
Others
|
(+)-Pinanediol ((1S,2S,3R,5S)-(+)-Pinanediol) is a potent inducer of melanin production. In S91 cells, it acts by inducing higher levels of pigmentation and nitric oxide (NO) synthesis [1].
|
-
- HY-P3137
-
|
Angiotensin Receptor
|
Cardiovascular Disease
|
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .
|
-
- HY-155481
-
|
Cannabinoid Receptor
|
Neurological Disease
|
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
|
-
- HY-112950
-
|
RET
|
Cancer
|
RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .
|
-
- HY-143735
-
|
RAD51
|
Cancer
|
RAD51-IN-4 is a potent inhibitor of RAD51. RAD51 is a eukaryote gene. RAD51-IN-4 has the potential for the research of conditions involving mitochondrial defects (extracted from patent WO2019014315A1, compound R12) .
|
-
- HY-17447B
-
-
- HY-163226
-
|
Ligands for E3 Ligase
Autophagy
|
Cancer
|
(1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-163227
-
|
Ligands for E3 Ligase
Autophagy
|
Cancer
|
(1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
|
-
- HY-P1810
-
|
Vasopressin Receptor
|
Neurological Disease
|
c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm is a is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.25 and 0.05 nM for hV2R and rV2R, respectively .
|
-
- HY-120242
-
|
Antibiotic
|
Infection
|
N-(3-Oxobutanoyl)-L-homoserine lactone (3-oxo-C4-HSL) is a carbapenem antibiotic biosynthesis autoregulator in Erwinia carotovora ATCC 39048. N-(3-Oxobutanoyl)-L-homoserine lactone induces expression of rhiI in R. leguminosarum .
|
-
- HY-E70533
-
|
Complement System
|
Inflammation/Immunology
|
C1r proenzyme, the native form of C1r enzyme, is an inactive zymogen until C1 is activated. C1r is activated when C1 binds to and is activated by antibodies bound to antigens (immune complexes) yielding C1r enzyme .
|
-
- HY-14794A
-
(1S,2R)-Milnacipran; F2695
|
Serotonin Transporter
|
Metabolic Disease
|
Levomilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Levomilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
|
-
- HY-14794
-
(1R,2S)-milnacipran; F2696
|
Serotonin Transporter
|
Metabolic Disease
|
Dextromilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Dextromilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1).
|
-
- HY-138996
-
|
GCGR
|
Metabolic Disease
|
GLP-1 receptor agonist 8 is a potent agonist of GLP-1 R. GLP-1 receptor agonist 8 has the potential for the research of diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD) (extracted from patent WO2019239319A1, compound 17) [1].
|
-
- HY-N0742
-
|
Others
|
Others
|
Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca 2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46 .
|
-
- HY-101768
-
PRN1371
1 Publications Verification
|
FGFR
c-Fms
|
Cancer
|
PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively .
|
-
- HY-13038A
-
R788
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-157422
-
|
c-Fms
|
Cancer
|
CSF1R-IN-19 is a potent inhibitor of CSF1R. CSF1R-IN-19 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-19 has the potential for the research of cancer [1].
|
-
- HY-116439
-
DINP
|
Angiotensin Receptor
|
Cardiovascular Disease
|
Diisononyl phthalate (DINP) is a phthalate used as a plasticizer. Diisononyl phthalate induces an increase in blood pressure through activation of the ACE/AT1R axis and inhibition of NO production in mice. Diisononyl phthalate can also be used in resin solvents, building materials, lubricants, adhesives, cosmetics and printing inks [1].
|
-
- HY-P1809
-
c(Bua-Cpa-Thi-Val-ASn-Cys)-Pro-d-Arg-NEt2
|
Vasopressin Receptor
|
Metabolic Disease
|
Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively .
|
-
- HY-13038B
-
R788 disodium hexahydrate
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-10002B
-
(1R,5Z)-1,25-Dihydroxyvitamin D3
|
VD/VDR
|
Cancer
|
(1R,5Z)-Calcitriol ((1R,5Z)-1,25-Dihydroxyvitamin D3) is a Calcitriol (HY-10002) isomer. Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist [1].
|
-
- HY-156113
-
|
RET
|
Cancer
|
RET-IN-25 (compound 6b) is a RET kinase inhibitor with anticancer activity. RET-IN-25 inhibits medullary thyroid carcinoma (MTC) with IC50s of 3.6 μM (3 days) and 3.0 μM (6 days) against TT(C634R) MTC .
|
-
- HY-169084
-
|
Glycosyltransferase
|
Cancer
|
ST-IN-1 (compound (R)-1) is a selective ST inhibitor (Ki=70 nM, rat a-2,6-ST; Ki=19 nM, hST6GAL1) with antitumor activity. ST-IN-1 inhibits tumor growth and metastasis by delipidating the surface of tumor cells [1].
|
-
- HY-N2273
-
|
LXR
|
Metabolic Disease
|
Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br . Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression .
|
-
- HY-145308
-
-
- HY-13038
-
R788(Disodium)
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-151105
-
|
Cannabinoid Receptor
|
Neurological Disease
|
CBR Agonist-1 (27a-cis) is a cannabinoid receptor (CBR) agonist with the Ki values of 0.18 μM for CB1R and 1.22 μM for CB2R. CBR Agonist-1 (27a-cis) can be used in the study of endogenous cannabinoid system-related diseases [1].
|
-
- HY-P1809A
-
c(Bua-Cpa-Thi-Val-ASn-Cys)-Pro-d-Arg-NEt2 acetate
|
Vasopressin Receptor
|
Metabolic Disease
|
Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) acetate is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively .
|
-
- HY-150552
-
-
- HY-155155
-
|
SARS-CoV
Sigma Receptor
|
Infection
|
SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC50: 80 nM). SARS-CoV-2-IN-57 has high affinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively .
|
-
- HY-B0025
-
|
Glycosidase
|
Metabolic Disease
|
Voglibose is an orally active alpha-glucosidase inhibitor that prevents the development of colorectal precancerous lesions induced by obesity and diabetes. Voglibose reduces oxidative stress in an inflammatory environment and inhibits the insulin-like growth factor/insulin-like growth factor-1 receptor (IGF/IGF-1R) functional axis [1].
|
-
- HY-112801
-
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
|
Cancer
|
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively .
|
-
- HY-146874S
-
|
Isotope-Labeled Compounds
|
Others
|
D-myo-Inositol, 1-[(2R)-3-[(1-oxoheptadecyl)oxy]-2-[[(9Z)-1-oxo-9-hexadecen-1-yl]oxy]propyl hydrogen phosphate]-d5, ammonium salt (1:1) is an isotopically labeled compound.
|
-
- HY-P1858A
-
|
CRFR
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
|
-
- HY-126748
-
|
Histamine Receptor
|
Others
|
VUF14862 is a stable and fatigue-resistant photoswitchable GPCR antagonist targeting the histamine H3 receptor (H3R) pathway. VUF14862 binds to H3R with >10-fold increased affinity upon 360 nm irradiation. VUF14862 can be used for spatiotemporal studies of H3R signaling .
|
-
- HY-100449A
-
|
Prostaglandin Receptor
|
Endocrinology
|
(S)-AL 8810 is an 11β-fluoro analog of PGF2α that acts as a potent and selective antagonist at the FP receptor. (S)-AL 8810 is the C-15 epimer of AL 8810, having the
inverse, (S), or "natural" configuration at C-15 relative to AL 8810, which is 15-(R) .
|
-
- HY-146873S
-
|
Isotope-Labeled Compounds
|
Others
|
D-myo-Inositol, 1-[(2R)-3-[(1-oxoheptadecyl)oxy]-2-[[(9Z)-1-oxo-9-tetradecen-1-yl]oxy]propyl hydrogen phosphate]-d5, ammonium salt (1:1) is an isotopically labeled compound.
|
-
- HY-P1858
-
|
CRFR
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
|
-
- HY-155706
-
|
Opioid Receptor
Dopamine Receptor
|
Inflammation/Immunology
|
MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism .
|
-
- HY-15772S1
-
AZD-9291-13C,d3; Mereletinib-13C,d3
|
EGFR
|
Cancer
|
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
|
-
- HY-15772
-
Osimertinib
Maximum Cited Publications
118 Publications Verification
AZD-9291; Mereletinib
|
EGFR
|
Cancer
|
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer [1].
|
-
- HY-15772A
-
AZD-9291 mesylate; Mereletinib mesylate
|
EGFR
|
Cancer
|
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer [1].
|
-
- HY-P3291
-
ZP7570
|
GCGR
|
Metabolic Disease
|
Dapiglutide (ZP7570) is a long-acting glucagon-like peptide-1 receptor 1R (GLP-1R)/Glucagon-like peptide-2 receptor (GLP-2R) dual agonist. Dapiglutide alleviates intestinal dysfunction in a mouse short bowel model and has anti-obesity effects [1] .
|
-
- HY-13631J
-
(1R,9R)-DX8951f
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
(1R,9R)-Exatecan mesylate((1R,9R)-DX8951f) is an isomer of Exatecan mesylate (HY-13631A). Exatecan mesylate (DX8951f) is an inhibitor of DNA topoisomerase I with an IC50 of 2.2 μM (0.975 μg/mL) and can be used in cancer research [1].
|
-
- HY-108618
-
BC11-38
1 Publications Verification
|
Phosphodiesterase (PDE)
|
Endocrinology
|
BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells .
|
-
- HY-149387
-
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
- HY-N0742R
-
|
Others
|
Others
|
Absinthin (Standard) is the analytical standard of Absinthin. This product is intended for research and analytical applications. Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46 .
|
-
- HY-P99259
-
FPA 008; Anti-Human CSF1R Recombinant Antibody
|
c-Fms
|
Inflammation/Immunology
Cancer
|
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances T cell infiltration and antitumor T cell immune responses. Cabiralizumab inhibits the activation of osteoclasts and blocks bone destruction, and can be used in the research of rheumatoid arthritis (RA). Cabiralizumab can combine with Nivolumab (HY-P9903) for lung cancer research [1] .
|
-
- HY-149386
-
|
Dopamine Receptor
Opioid Receptor
|
Inflammation/Immunology
|
D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
|
-
- HY-168065
-
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Keap1-Nrf2-IN-22 (compound 19) is a Keap1-Nrf2 inhibitor, with a KD2 value of 42.2 nM for Keap1. Keap1-Nrf2-IN-22 can be used for the study of acute lung injury (ALI) and cerebral ischemia/reperfusion (I/R) injury .
|
-
- HY-13038AR
-
|
Syk
FLT3
|
Inflammation/Immunology
Cancer
|
Fostamatinib (Standard) is the analytical standard of Fostamatinib. This product is intended for research and analytical applications. Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
|
-
- HY-125527A
-
17(R)-RvD1; AT-RvD1
|
TRP Channel
|
Inflammation/Immunology
|
17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells [1]. 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
|
-
- HY-15772S
-
AZD-9291-d6; Mereletinib-d6
|
EGFR
|
Cancer
|
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
|
-
- HY-114076
-
|
GABA Receptor
|
Neurological Disease
|
CGP55845 is a potent and selective GABAB receptor antagonist with activity that blocks agonist binding. The IC50 value of CGP55845 is 5 nM, indicating that it exhibits significant activity in inhibiting GABA and glutamate release. The apparent Kd of CGP55845 when forming a complex with the GABAB receptor is 30 nM, indicating its high affinity for this receptor. CGP55845 is as potent as 100 μM CGP 35348 in relieving the inhibitory effect of (R)-(-)-baclofen .
|
-
- HY-121835
-
|
GCGR
|
Metabolic Disease
|
GLP-1R agonist 2 (compound 2) is an effective GLP-1R agonist that exerts its activating effect by forming hydrogen bonds with the Tyr42, Cys71, and Ser84 residues of GLP-1R. GLP-1R agonist 2 has the potential for research in metabolic diseases such as type 2 diabetes and obesity [1].
|
-
- HY-14176A
-
|
γ-secretase
|
Cancer
|
(1R,3S)-Compound E is the isomer of Compound E (HY-14176), and can be used as an experimental control. Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
|
-
- HY-116603
-
|
5-HT Receptor
|
Others
|
SB-236057 is an inverse agonist of the 5-HT1B receptor that exhibits strong skeletal teratogenicity in rodents and rabbits. SB-236057 affects gene expression during embryonic development through interference with the Notch signaling pathway and interaction with r-esp1. SB-236057 induces somatic patterning and tail extension defects in rat embryos during early organogenesis [1].
|
-
- HY-P99189
-
IMC-A12; NSC742460
|
IGF-1R
|
Cancer
|
Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with high affinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer [1].
|
-
- HY-109001A
-
(1S,2R)-ABT-957
|
Proteasome
|
Neurological Disease
|
(1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD) [1]. (1S,2R)-Alicapistat mitigates the metabolic liability of carbonyl reduction and inhibits calpain 1 with an IC50 value of 395 nM .
|
-
- HY-148365
-
|
Mixed Lineage Kinase
RIP kinase
CDK
|
Cancer
|
NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin (HY-17394)-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression [1].
|
-
- HY-103277A
-
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
BIM 23042 TFA, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release [1] .
|
-
- HY-103277
-
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release [1] .
|
-
- HY-15772AR
-
|
EGFR
|
Cancer
|
Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer [1].
|
-
- HY-15772R
-
|
EGFR
|
Cancer
|
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer [1].
|
-
- HY-122171
-
|
Histamine Receptor
|
Neurological Disease
|
A-317920 is a selective and potent rat histamine H3 receptor (H3R) antagonist with pKi value of 9.2 and 7.0 for full-length rat and full-length human H3R, respectively. A-317920 exhibits over 130 fold selective affinity for the rat over the human H3R. A-317920 enhances cognition via H3R blockade .
|
-
- HY-W007978
-
R-(-)-2,2-Diamino-1,1-binaphthyl
|
Biochemical Assay Reagents
|
Others
|
(R)-[1,1'-Binaphthalene]-2,2'-diamine is the isomer of (S)-[1,1'-Binaphthalene]-2,2'-diamine (HY-W007978A), and can be used as an experimental control. (S)-[1,1'-Binaphthalene]-2,2'-diamine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-109114A
-
MT-7117 phosphate
|
Melanocortin Receptor
|
Metabolic Disease
|
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 [1] .
|
-
- HY-170974
-
|
Fungal
|
Infection
|
SDH-IN-20 (compound A19) is an antifungal agent. SDH-IN-20 against Verticillium dahlia, R. solani with EC50s of less than 3.0 μg/mL, 2.87 μg/mL. SDH-IN-20 exerts its highly antifungal effects by acting as an effective succinate dehydrogenase (SDH) inhibitor with an IC50 of 29.33 μM. SDH-IN-20 adversely impacts the integrity of cell membranes and mycelial morphologies of R. solani .
|
-
- HY-103320B
-
|
CaSR
|
Metabolic Disease
|
(1R,2R)-Calhex 231 hydrochloride is the isomer of Calhex 231 hydrochloride (HY-103320A), and can be used as an experimental control. Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment [1] .
|
-
- HY-14794AS
-
(1S,2R)-Milnacipran-d10 hydrochloride; F2695-d10 hydrochloride
|
Isotope-Labeled Compounds
Serotonin Transporter
|
Metabolic Disease
|
Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran. Levomilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Levomilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1) [1].
|
-
- HY-155967
-
|
AMPK
Cannabinoid Receptor
|
Metabolic Disease
|
CB1R/AMPK modulator 1 (Compound 38-S) is an orally active CB1R/AMPK modulator, with an Ki of 0.81 nM and an IC50 of 3.9 nM for CB1R. CB1R/AMPK modulator 1 activates AMPK. CB1R/AMPK modulator 1 reduces food intake and body weight, and improves glucose tolerance and insulin sensitivity [1].
|
-
- HY-122294
-
|
Endogenous Metabolite
|
Neurological Disease
|
Rociverine is an anticholinergic compound with smooth muscle relaxant activity. Rociverine showed different binding modes in five cloned muscarinic receptors. The cis stereoisomer of Rociverine showed a higher affinity change compared to the trans stereoisomer. The (1R,2R) configuration of Rociverine showed significantly higher affinity, even up to 240 times. The (1S,2S) configuration of Rociverine is very important for binding selectivity [1].
|
-
- HY-163854
-
|
HSP
Bcl-2 Family
Apoptosis
|
Cancer
|
HSP70-IN-6 (Compound JL-15) is an inhibitor of Hsp70-Bim protein-protein interaction (PPI) (IC50: 70 nM). HSP70-IN-6 induces apoptosis in chronic myeloid leukemia (CML) cells, with EC50s of 0.43 μM(BV173), 0.88 μM (K562), 0.19 μM (K562-R3) .
|
-
- HY-P4146
-
BI 456906
|
GLP Receptor
GCGR
|
Metabolic Disease
|
Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake [1].
|
-
- HY-P5875
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
|
-
- HY-144034
-
|
GCGR
|
Metabolic Disease
|
GLP-1R agonist 3 is a potent agonist of GLP-1R. GLP-1R agonist 3 is a thickened imidazole derivative compound. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 3 has the potential for the research of diabetes (extracted from patent WO2021197464A1, compound 1) [1].
|
-
- HY-100218B
-
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
(1R,3S)-RSL3 is the less active (1R,3S)-enantiomer of RSL3 ((1S,3R)-RSL3). (1R,3S)-RSL3 and RSL3 induce cell death in HT22 wild-type cells with EC50 values of 5.2 µM and 0.004 µM, rspectively [1].
|
-
- HY-P4146A
-
BI 456906 TFA
|
GLP Receptor
GCGR
|
Metabolic Disease
|
Survodutide (BI 456906) TFA is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake [1].
|
-
- HY-109114
-
MT-7117
|
Melanocortin Receptor
|
Metabolic Disease
|
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 [1] .
|
-
- HY-50905
-
CHIR-258; TKI258
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity [1] .
|
-
- HY-150025
-
|
DNA Methyltransferase
Apoptosis
|
Cancer
|
(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 .
|
-
- HY-P1205
-
Melanin-concentrating hormone(human, mouse, rat)
|
MCHR1 (GPR24)
|
Neurological Disease
|
MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively .
|
-
- HY-144041
-
|
c-Fms
|
Cancer
|
CSF1R-IN-5 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-5 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-5 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 11) [1].
|
-
- HY-144040
-
|
c-Fms
|
Cancer
|
CSF1R-IN-4 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-4 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-4 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 104) [1].
|
-
- HY-P1205A
-
Melanin-concentrating hormone(human, mouse, rat) TFA
|
MCHR1 (GPR24)
|
Neurological Disease
|
MCH (human, mouse, rat) TFA is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively .
|
-
- HY-144042
-
|
c-Fms
|
Cancer
|
CSF1R-IN-6 is a potent inhibitor of CSF1R. CSF-1R is expressed in macrophages, and the survival and differentiation of macrophages depends on the CSF-1/CSF-1R signaling pathway. CSF1R-IN-6 affects the exchange of inflammatory factors between TAMs and glioma cells. CSF1R-IN-6 has the potential for the research of cancer disease (extracted from patent WO2021197276A1, compound 5) [1].
|
-
- HY-P5875A
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models .
|
-
- HY-101335
-
|
mGluR
|
Neurological Disease
|
DCG-IV is a potent agonist of group II mGluRs with EC50s of 0.35 and 0.09 μM for mGlu2R and mGlu3R, reapectively. DCG-IV is also a competitive antagonist at group I (IC50: mGlu1R/5R=389/630 μM) and III receptors (IC50: mGlu4R/6R/7R/8R= 22.5/39.6/40.1/32 μM). DCG-IV has anticonvulsive and neuroprotective effects [1] .
|
-
- HY-12215
-
PF-06463922
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-135509
-
PF-06463922 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-10624
-
THIQ
1 Publications Verification
|
Melanocortin Receptor
|
Metabolic Disease
|
THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
|
-
- HY-12215R
-
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-P1110
-
AF12198
3 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo [1].
|
-
- HY-170828
-
|
PROTACs
SWI/SNF Complex
|
Others
|
SMD-1087 is a PROTAC that selectively targets SMARCA2 (DC50=8 nM, Dmax=89%) and SMARCA4 with a DC50 of 1 μM. SMD-1087 consists of the E3 ligase ligand (S,R,S)-AHPC-Me (blue part) (HY-112078), the target protein ligand SMI-1074 (red part) (HY-170817), and the PROTAC linker (1r,4r)-tert-Butyl 4-(bromomethyl)cyclohexanecarboxylate (black part) (HY-W890392). Among them, its target protein ligand + Linker part corresponds to SMARCA2 Ligand-Linker Conjugate-1 (HY-170829) [1].
|
-
- HY-108495
-
ML248
|
LPL Receptor
|
Cardiovascular Disease
|
CYM50308 (ML248) is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM [1].
|
-
- HY-122575
-
|
P2X Receptor
Influenza Virus
Topoisomerase
MicroRNA
Apoptosis
|
Infection
Neurological Disease
Inflammation/Immunology
|
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
|
-
- HY-15616
-
|
Melanocortin Receptor
|
Cancer
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-I0718
-
|
Biochemical Assay Reagents
|
(R)-(-)-1,1'-Binaphthyl-2,2'-diyl Hydrogenphosphate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-20074
-
(1S,2S,3R,5S)-(+)-Pinanediol
|
Biochemical Assay Reagents
|
(+)-Pinanediol ((1S,2S,3R,5S)-(+)-Pinanediol) is a potent inducer of melanin production. In S91 cells, it acts by inducing higher levels of pigmentation and nitric oxide (NO) synthesis [1].
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99004
-
|
Melanocortin Receptor
|
Inflammation/Immunology
|
(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family [1].
|
-
- HY-W045221
-
-
- HY-P1504
-
-
- HY-P1504A
-
-
- HY-19870
-
-
- HY-149941
-
|
Neurotensin Receptor
|
Neurological Disease
|
hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent [1].
|
-
- HY-P4745
-
|
MCHR1 (GPR24)
|
Metabolic Disease
|
hMCH-1R antagonist 1 (Compound 30) is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM. HMCH-1R antagonist 1 can bind to hMCHR1 and hMCHR2 with IC50 values of 65 nM and 49 nM, respectively. HMCH-1R antagonistist 1 can be used for metabolic research [1].
|
-
- HY-P3359
-
-
- HY-P4043
-
|
HBV
|
Infection
Inflammation/Immunology
|
Hepatitis b virus pre-s region (120-145) is a preS2 peptide that inhibits the binding of single-chain Fv fragment (scFv) or IgG to r-HBsAg .
|
-
- HY-P4386
-
|
GLP Receptor
|
Metabolic Disease
|
(Asp28)-Exenatide is a degradation product of exenatide (HY-13443). (Asp28)-Exenatide can be used as a GLP-1R agonist .
|
-
- HY-19870A
-
-
- HY-P10474
-
|
Drug Isomer
|
Others
|
RYTVELA is a deriviative of the peptide antagonist of interleukin-1 receptor 1 (IL-1R1) d-(RYTVELA) (HY-P10353) that contains all L-amino acids [1].
|
-
- HY-P10827
-
|
Complement System
|
Inflammation/Immunology
|
PIC1 PA, a 15 amino-acid peptide, is a potent PIC1 analog that inhibits classical pathway mediated complement activation. PIC1 PA functionally disrupts the C1s-C1r-C1r-C1s/MASPs interaction with collagen-like region (CLR) of C1q/MBL, respectively. PIC1 PA specifically binds to the CLR of C1q and bounds to purified C1q with a mean equilibrium dissociation constant (KD) of 33.3 nM [1].
|
-
- HY-P4385
-
|
PTHR
|
Metabolic Disease
|
(Asn10,Leu11,D-Trp12)-pTH-Related Protein (7-34) amide (human, mouse, rat) is a potent PTH-1R antagonist .
|
-
- HY-P3137
-
|
Angiotensin Receptor
|
Cardiovascular Disease
|
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .
|
-
- HY-P1810
-
|
Vasopressin Receptor
|
Neurological Disease
|
c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-Agm is a is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.25 and 0.05 nM for hV2R and rV2R, respectively .
|
-
- HY-P1809
-
c(Bua-Cpa-Thi-Val-ASn-Cys)-Pro-d-Arg-NEt2
|
Vasopressin Receptor
|
Metabolic Disease
|
Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively .
|
-
- HY-P1809A
-
c(Bua-Cpa-Thi-Val-ASn-Cys)-Pro-d-Arg-NEt2 acetate
|
Vasopressin Receptor
|
Metabolic Disease
|
Velmupressin (c(Bua-Cpa-Thi-Val-Asn-Cys)-Pro-d-Arg-NEt2) acetate is a potent, selective and short-acting peptidic V2 receptor (V2R) agonist with EC50s of 0.07 and 0.02 nM for hV2R and rV2R, respectively .
|
-
- HY-P1858A
-
|
CRFR
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Urocortin III, mouse TFA is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
|
-
- HY-P1858
-
|
CRFR
|
Cardiovascular Disease
Neurological Disease
Endocrinology
|
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2 . Urocortin III (Ucn3) is a known component of the behavioral stress response system. Urocortin III and CRF-R2 in the medial amygdala regulate complex social dynamics .
|
-
- HY-P3291
-
ZP7570
|
GCGR
|
Metabolic Disease
|
Dapiglutide (ZP7570) is a long-acting glucagon-like peptide-1 receptor 1R (GLP-1R)/Glucagon-like peptide-2 receptor (GLP-2R) dual agonist. Dapiglutide alleviates intestinal dysfunction in a mouse short bowel model and has anti-obesity effects [1] .
|
-
- HY-103277A
-
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
BIM 23042 TFA, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release [1] .
|
-
- HY-103277
-
|
Bombesin Receptor
|
Neurological Disease
Metabolic Disease
|
BIM 23042, a certain somatostatin (SS) octapeptide analogue, is a selective neuropeptide neuromedin B receptor (NMB-R, BB1) antagonist. BIM 23042 has 100-fold lower affinity for gastrin-releasing peptide (GRP) receptor (BB2). BIM 23042 inhibits Neuromedin B (HY-P0241), ICI 216140 and DPDM-bombesin ethylamide-induced Ca 2+ release [1] .
|
-
- HY-P4146
-
BI 456906
|
GLP Receptor
GCGR
|
Metabolic Disease
|
Survodutide (BI 456906) is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake [1].
|
-
- HY-P5875
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
|
-
- HY-P4146A
-
BI 456906 TFA
|
GLP Receptor
GCGR
|
Metabolic Disease
|
Survodutide (BI 456906) TFA is a potent, selective glucagon receptor/GLP-1 receptor (GCGR/GLP-1R) dual agonist with EC50s of 0.52 nM and 0.33 nM in CHO-K1 cells, respectively. Survodutide TFA, a 29-amino-acid peptide, is a potent acylated peptide containing a C18 fatty acid. Survodutide TFA has robust anti-obesity efficacy achieved by increasing energy expenditure and decreasing food intake [1].
|
-
- HY-P1205
-
Melanin-concentrating hormone(human, mouse, rat)
|
MCHR1 (GPR24)
|
Neurological Disease
|
MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively .
|
-
- HY-P1205A
-
Melanin-concentrating hormone(human, mouse, rat) TFA
|
MCHR1 (GPR24)
|
Neurological Disease
|
MCH (human, mouse, rat) TFA is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively .
|
-
- HY-P5875A
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models .
|
-
- HY-P1110
-
AF12198
3 Publications Verification
|
Interleukin Related
|
Inflammation/Immunology
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo [1].
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990084
-
|
IGF-1R
|
Cancer
|
Veligrotug is an IgG1-kappa, anti-IGF1R (insulin-like growth factor 1 receptor, CD221) chimeric monoclonal antibody [1].
|
-
- HY-P99712
-
hz208F2-4
|
IGF-1R
ADC Antibody
|
Cancer
|
Lonigutamab (hz208F2-4) is a humanized anti-IGF-1R monoclonal antibody that can be used for the synthesis of antibody–agent conjugates (ADC) [1].
|
-
- HY-P99259
-
FPA 008; Anti-Human CSF1R Recombinant Antibody
|
c-Fms
|
Inflammation/Immunology
Cancer
|
Cabiralizumab (FPA 008) is an anti-CSF1R monoclonal antibody (MAb). Cabiralizumab enhances T cell infiltration and antitumor T cell immune responses. Cabiralizumab inhibits the activation of osteoclasts and blocks bone destruction, and can be used in the research of rheumatoid arthritis (RA). Cabiralizumab can combine with Nivolumab (HY-P9903) for lung cancer research [1] .
|
-
- HY-P99189
-
IMC-A12; NSC742460
|
IGF-1R
|
Cancer
|
Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with high affinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer [1].
|
-
- HY-P990844
-
|
Complement System
|
Others
|
Anti-GC1q R/C1QBP Antibody (60.11) is a kind of mouse IgG1, κ chimeric antibody, targeting to human GC1q R/C1QBP. The recommend isotype control of Anti-GC1q R/C1QBP Antibody (60.11): Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
- HY-P990871
-
|
Integrin
|
Others
|
Anti-CD11a/LFA-1α Antibody (R7-1) is a kind of mouse IgG1 chimeric antibody, targeting to human CD11a/LFA-1α. The recommend isotype control of Anti-CD11a/LFA-1α Antibody (R7-1): Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
- HY-P990777
-
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0317DS
-
|
(R)-Amlodipine-d4 is the deuterium labeled (R)-Amlodipine[1].
|
-
-
- HY-142165S
-
|
(R)-Norverapamil-d6 (hydrochloride) is deuterium labeled (R)-Norverapamil .
|
-
-
- HY-14519CS
-
|
(R)-Methotrexate-d3 is the deuterium labeled (R)-Methotrexate[1].
|
-
-
- HY-B0573CS
-
|
(R)-Propranolol-d7 is the deuterium labeled (R)-Propranolol[1].
|
-
-
- HY-14948S1
-
|
(R)-Carisbamate-d4 is the deuterium labeled (R)-Carisbamate[1].
|
-
-
- HY-133171AS3
-
|
(R)-Norfluoxetine-d5 is the deuterium labeled (R)-Norfluoxetine[1].
|
-
-
- HY-143777S
-
|
(R)-Etodolac-d4 is the deuterium labeled (R)-Etodolac[1].
|
-
-
- HY-170006S
-
|
9(R)-Hexahydrocannabinol-d9 is deuterium labeled 9(R)-Hexahydrocannabinol .
|
-
-
- HY-158187S
-
|
R-(+)-Cibenzoline-d4 (R-(+)-Cifenline-d4) is deuterium labeled R-(+)-Cibenzoline ((R-(+)-Cifenline) .
|
-
-
- HY-125527AS
-
|
17(R)-Resolvin D1-d5 (17(R)-RvD1-d5) is deuterium labeled 17(R)-Resolvin D1. 17R-Resolvin D1 (17R-RvD1; AT-RvD1) is an aspirin-triggered epimer of Resolvin D1, which exhibits anti-inflammatory activity in mice and human PMNs cells [1]. 17R-Resolvin D1 specificially inhibits TRPV3 with an IC50 of 398 nM and exhibits peripheral anti-nociceptive efficacy .
|
-
-
- HY-146874S
-
|
D-myo-Inositol, 1-[(2R)-3-[(1-oxoheptadecyl)oxy]-2-[[(9Z)-1-oxo-9-hexadecen-1-yl]oxy]propyl hydrogen phosphate]-d5, ammonium salt (1:1) is an isotopically labeled compound.
|
-
-
- HY-146873S
-
|
D-myo-Inositol, 1-[(2R)-3-[(1-oxoheptadecyl)oxy]-2-[[(9Z)-1-oxo-9-tetradecen-1-yl]oxy]propyl hydrogen phosphate]-d5, ammonium salt (1:1) is an isotopically labeled compound.
|
-
-
- HY-15772S1
-
|
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
|
-
-
- HY-15772S
-
|
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
|
-
-
- HY-14794AS
-
|
Levomilnacipran-d10 ((1S,2R)-Milnacipran-d10) hydrochloride is deuterium labeled Levomilnacipran. Levomilnacipran (F2696; (1R,2S)-milnacipran), an enantiomer of milnacipran, is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. Levomilnacipran also is a human alpha-adrenergic receptor antagonist, with an IC50 of 3.4 μM. (patent WO2013014263A1) [1].
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-155481A
-
|
|
Azide
|
CB2 receptor antagonist 4 (compound (R)-1) is a CB2R-selective inverse agonist with a Kd value of 39 nM [1].
|
-
- HY-155481
-
|
|
Azide
|
CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: