Catalog No.
Product Name
Application
Product Information
Citations
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NMDA& mGlu receptor agonist
Ibotenic acid is a neuroexcitatory amino acid originally isolated from Amanita species that functions as a NMDA and metabotropic glutamate receptor agonist. -
5-HT6 serotonin receptor antagonist
SB 258585 hydrochloride has been found to be a selective and potent SR-6 antagonist. This compound displays more than a 160-fold selectivity over other serotonin receptor subtypes. -
CRF-1 antagonist
Emicerfont, also known as GW876008, is a CRF-1 antagonist. Emicerfont blocks the CRH-1 receptor, and so reduces ACTH release. -
GLP-1 receptor agonist
ixisenatide inhibit glucagon release, markedly reduce postprandial glucago. have a promoting effct in diabetes mellitus (T2DM). - Bifeprunox Mesylate is an antipsychotic compound through activation of the serotonin 5-hydroxytryptamine (5-HT)1A receptor.
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5-HT6 antagonist
SB 399885 hydrochloride 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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OX2 receptor antagonist
JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 μM for OX1R). -
CRF1 receptor antagonist
Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1??0.6 nM for human CRF1 receptor. -
angiotensin II receptor antagonist
BIBS39 is a nonpeptide angiotensin II (AII) receptor antagonists that displaced [125I] AII from its specific binding sites with a K(i) value of 29 +/- 7 nM for the AII subtype I (AT1) receptor and a K(i) value of 480 +/- 110 nM for the AII subtype 2 (AT2) receptor. -
Adenosine Receptor agonist
Capadenoson is a selective agonist of adenosine-A1 receptor. -
5-HT6 agonist
WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM. -
dopaminergic agonist
Pergolide mesylate is a dopaminergic agonist that also decrease plasma prolactin concentrations. -
LPA1 Receptor antagonist
AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively -
CB2 receptor agonist
Tedalinab (GRC-10693) is a drug developed for the treatment of osteoarthritis and neuropathic pain, which acts as a potent and selective cannabinoid CB2 receptor agonist. It has a very high selectivity of 4700x for CB2 over the related CB1 receptor, has good oral bioavailability and has shown promising safety results and effective analgesic and antiinflammatory actions in early clinical trials. -
CXCR2 antagonist
SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury. -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
β2-adrenoceptor agonist
Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effect. -
Histamine H1 receptor antagonist
Promethazine HCl is a potent histamine H1 receptor antagonist. -
β-adrenoceptor agonist
Bambuterol HCl is a potent β-adrenoceptor agonist, used in the treatment of asthma. -
5-HT2 receptor antagonist
Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations. -
I(1) imidazoline receptor agonist
Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist. -
mGluR-2 modulator
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 receptor. -
neuropeptide Y Y2 receptor antagonist
JNJ-31020028 is a novel, selective, brain-penetrant neuropeptide Y Y2 receptor antagonist - Capromorelin functions as a growth hormone secretagogue and ghrelin mimetic which causes the body to secrete human growth hormone in a way usually seen at puberty and in young adulthood.
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ETBR antagonist
BQ-788 sodium salt is a selective ETBR (Endothelin receptor B ) antagonist. -
5-HT3 receptor antagonist
Tropisetron is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ?? 0.9 nM for 5-HT3 receptor. -
Dopamine receptor agonist
(+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM). -
serotonin/NE reuptake inhibitor
Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor. -
Adenosine A3 receptor agonist
CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. -
NK1 receptor antagonist
Netupitant is a selective neurokinin 1 (NK1) receptor antagonist. It competitively binds to and blocks the activity of the human substance P/NK1 receptors in the central nervous system (CNS), thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in the prevention of chemotherapy-induced nausea and vomiting (CINV). -
5-HT2A receptor agonist
Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay. -
FFA4/GPR120 agonist
GSK137647A is a selective FFA4 agonist, with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively. -
5-HT1F antagonist
LY 334370 hydrochloride is a selective 5-HT1F receptor agonist (Ki values are 1.87, 16.4, > 100 (IC50)). CAS: 199673-74-0(LY 334370 hydrochloride); 182563-08-2 (LY 334370 Free Base)
