Catalog No.
Product Name
Application
Product Information
Citations
-
oxytocin receptor antagonist
L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively, used as a tocolytic agent. -
neuropeptide Y5 receptor antagonist
CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes. -
NK2 antagonist
GR 159897 is a highly potent, selective, competitive, brain-penetrated non-peptide antagonist at tachykinin NK2 receptors, inhibits binding of [3H]GR100679 to hNK2-CHO cells and rat colon membranes with pKis of 9.51 and 10, respectively. Antagonizes bronchoconstriction, with anxiolytic-like activity. -
GLP-1 receptor agonist
GLP-1 receptor agonist 1 is a glucagon-like peptide-1 (GLP-1) receptor agonist extracted from patent WO2018056453A1, Compound 67. -
peripheral adrenoceptor antagonist
Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors. -
CB1 agonist
Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status. -
Adenosine receptor agonist
N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively. -
melatonin agonist
Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist. -
MCHR1 antagonist
SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. -
peptidoleukotrienes antagonist
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M. -
Oxytocin antagonist
OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM. -
oxytocin (OT) antagonist
OT antagonist 3 is an oxytocin (OT) antagonist extracted from patent WO2007017752A1. -
AT1 receptor antagonist
ZD 7155 hydrochloride is an angiotensin II receptor type 1 (AT1 receptor) antagonist. -
γ-L-Glutamyl-L-alanine, composed of gamma-glutamate and alanine, is a proteolytic breakdown product of larger proteins.
-
5-HT4 receptor antagonist
Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities. -
GPR35/CXCR8 agonist
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8. -
NOP agonist
MT-7716 hydrochloride (W-212393 hydrochloride) is a selective non-peptide nociceptin receptor (NOP) agonist and promising potential treatment drug for alcohol abuse and relapse prevention. -
A1 adenosine receptor agonist
N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist. -
β adrenergic receptor antagonist
Pargolol hydrochloride is a β adrenergic receptor antagonist. -
histamine H3 receptor antagonist
Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder. -
EP4 partial agonist
GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC50 of 7.4. -
GPR40/FFAR1 agonist
GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1). - GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
-
5-HT7 receptor agonist
5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders. -
5-HT3 /5-HT4 receptor dual antagonist
FK1052 hydrochloride is a potent 5-HT3 and 5-HT4 receptor dual antagonist. -
adenosine receptor antagonist
Taminadenant is an antagonist of adenosine receptor.
