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MC1R and MC5R antagonist
JNJ-10229570 is a novel MC1R and MC5R antagonist was used to treat primary human sebaceous cells. -
α1A antagonist
RS 17053 HCl is α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8). -
Endogenous galanin receptor agonist
Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects -
NK1 receptor antagonist
Tradipitant, also known as VLY-686 and LY686017, is the 2nd generation neurokinin-1 receptor antagonist, which showed activity in preclinical anxiety models. -
KOR agonist
Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively). -
CGRP receptor antagonist
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
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CRF-1 antagonist
Verucerfont, also known as GSK561679 and NBI77860, is a CRF-1 antagonist. Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress. -
5-HT6 receptor antagonist
SB 399885 is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).
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DP1 receptor antagonist
Asapiprant, also known as S-555739, is a the potent and selective DP1 receptor antagonist. Asapiprant exhibited high affinity and selectivity for the DP1 receptor. - Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
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CXCR2 receptor antagonist
Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor. -
δ opioid receptor antagonist
Naltrindole hydrochloride is a highly potent and selective non-peptide δ opioid receptor antagonist with a Ki of 0.02 nM. -
mGlu1 receptor antagonist
JNJ16259685 is a selective antagonist of mGlu1 receptor, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM. -
mGlu1 receptors modulator
Ro 67-7476 is a positive allosteric modulator of mGlu1 receptors. -
mGluR agonist
L-Cysteinesulfinic acid is a potent agonist at several rat metabotropic glutamate receptors (mGluRs) with pEC50s of 3.92±0.03, 4.6±0.2, 3.9±0.2, 2.7±0.2, 4.0±0.2, and 3.94±0.08 for mGluR1, mGluR5, mGluR2, mGluR4, mGluR6, and mGluR8, respectively. -
guanylate cyclase stimulator
Nelociguat (BAY60-4552) is a nitric oxide sensitive soluble guanylate cyclase stimulator. -
EP2 receptor agonist
Taprenepag isopropyl is a highly selective EP2 receptor agonist. -
glucagon receptor antagonist
PF-06291874 (Glucagon receptor antagonists-4) is a highly potent and orally active glucagon receptor antagonist. It displays low in vivo clearance in both rats and dogs. -
glucagon receptor antagonist
Adomeglivant is a potent and selective glucagon receptor antagonist that is used in clinical trial for type 2 diabetes mellitus. -
μ-opioid receptor (MOR) antagonist
GSK1521498 is a potent and selective μ-opioid receptor (MOR) antagonist. GSK1521498 is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. - Aminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 (ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.
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5-HT7 receptor antagonist
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively. -
dopamine D2 receptor antagonist
Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor. -
glucagon-like peptide 1 receptor antagonist
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. -
5-HT3 partial agonist
Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease. -
triple tachykinin receptor antagonist
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows high affinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. -
NK3R antagonist
Fezolinetant is an antagonist of the neurokinin 3 receptor (NK3R), used for the treatment of menopausal hot flushes. -
PAF antagonist
Ro 24-4736 is a potent, selective, p.o.-active platelet-activating factor (PAF) antagonist with a long duration of action. -
thromboxane synthesis inhibitor
Ro-24-0238 is an antagonist of platelet activating factor (PAF) and inhibitor of thromboxane synthesis, used for lessening the inflammation and damage resulting from a local release of PAF. -
dual FPR1/FPR2/ALX agonist
FPR Agonist 43 (compound 43) is a dual formyl peptide receptor 1 (FPR1) and formyl peptide receptor 2 (FPR2)/ALX agonist.
GPCR/G Protein
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Application
Product Information
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