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Catalog No.
Product Name
Application
Product Information
Citations
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combined Ca2+/5-HT2 antagonist
Nexopamil racemate is the racemate of Nexopamil. Nexopamil is a combined Ca2+/5-HT2 antagonist on thrombus formation in vivo and on platelet aggregation in vitro. -
5-HT2 receptor antagonist
Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C). -
adenosine A3 receptor antagonist
MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM. -
histamine H1 receptor antagonist
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective ?? site (guinea pig brain) with Ki of 0.45 μM. -
PGF2α receptor antagonist
OBE022 is an oral and selective prostaglandin F2α (PGF2α) receptor antagonist, with Kis of 1 nM, 26 nM for human and rat FP receptors, respectively. -
H4R antagonist
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. -
CRTh2 antagonist
CRTh2 antagonist 1 is a CRTh2 antagonist with an IC50 of 89 nM. -
CGRP receptor antagonist
CGRP antagonist 1 is a highly potent CGRP receptor antagonist with a Ki and IC50 of 35 and 57 nM, respectively. -
neuropeptide Y1 receptor antagonist
Y1 receptor antagonist 1 (H 409-22 isomer) is a neuropeptide Y1 receptor antagonist. -
EP1 antagonist
EP1-antanoist-1 is a EP1 antagonist with a pKi of 7.54 and an pIC50 of 8.5. -
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. -
peripheral adrenoceptor antagonist
Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors. -
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. -
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. -
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. -
NK-1 receptor antagonist
NK-1 Antagonist 1 (Rolapitant intermediate) is an antagonist of NK-1 receptor, used in the research of NK-1 related diseases and conditions such as cough, overactive bladder, alcohol dependency and depression. -
MCH1 receptor antagonist
ALB-127158(a) is a potent and selective melanin concentrating hormone 1 (MCH1) receptor antagonist. -
SSTR5 antagonist
SSTR5 antagonist 1 is a potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively. (Compound 25a).
