Catalog No.
Product Name
Application
Product Information
Product Citation
-
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. -
alpha1/beta adrenergic receptors antagonist
Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
-
dopamine D2 receptor antagonist
Metoclopramide HCl is a selective dopamine D2 receptor antagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
-
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. -
OX1/OX2 Antagonist
Almorexant HCl is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor 3.- Ryan J Keenan, .et al. , Br J Pharmacol, 2022, Jul;179(13):3403-3417 PMID: 35112344
-
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 -
Adenosine A3-R agonist
IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.- Sameshima T, .et al. , Chem Res Toxicol, 2019, Aug 28 PMID: 31461269
- 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.
-
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. - Thrombin Receptor Activator for Peptide 5 (TRAP-5), coagulation factor II (thrombin) receptor is a G protein-coupled receptor involved in the regulation of thrombotic response.
- Corticotropin Releasing Factor, bovine, neurotransmitter and CRF receptor antagonist.
- Endothelin-2, human, endogenous peptide found predominately in the kidney and intestine. Displays similar selectivity for ETA and ETB endothelin receptors.
-
α1 receptor antagonist
Tamsulosin hydrochloride is a selective α1 receptor antagonist and a medicine which is used in benign prostatic hyperplasia. -
ET-A and ET-B antagonist
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. -
β2-adrenoceptor agonist
Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD). -
5HT3-receptor antagonist
Alosetron is s Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome. -
μ-opioid receptor agonist
Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery. -
μ-opioid receptor agonist
Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
