A 943931 dihydrochloride

A 943931, is an H4R (one of histamine receptor subtypes) antagonist with high affinities to H4Rs of human (Ki = 5 nM), rat (Ki = 4 nM) and mouse (Kb = 6 nM) . H4R is one of 4 known G-protein-coupled receptors (H1, H2, H3 and H4 receptors) of histamine for histamine to mediate its physiological functions . HMC-1 cells incubated with A 943931 at a concentration of 300 nM for 20 min inhibited the increase in ALDH2 activity induced by H4R . In microglia, A 943931 at a concentration of 10 μM partially abolish the release of TNF-α and IL-6 induced by histamine at a concentration of 0.1 μg/ml . In bone marrow-derived mast cells, A 943931 inhibited the shape change induced by histamine (IC50 = 0.38 μM) . Intraperitoneal administration of A 943931 at a dose of 33 μmol/kg potently inhibited itch induced by H4R agonist in mice . In several preclinical models, H4R had been shown to be linked to inflammation . A 943931 had excellent antagonistic activity both in vivo and in vitro across multiple species, displayed good oral bioavailability (90%) and excellent metabolic stability. This compound displays good efficacy in rat pain models and is a good anti-inflammatory agent in mice . A 943931 has an in vivo oral bioavailability of 34% and a half-life of 2.6 h in rats . A 943931 efficaciously reduced acute inflammatory pains induced by formalin in the flinch model and by carrageenan in mechanical and thermal hyperalgesia models in rats .

Product information

CAS Number: 1227675-50-4

Molecular Weight: 368.30

Formula: C17H23Cl2N5

Chemical Name: (3R)-1-{4-imino-3,5-diazatricyclo[9.4.0.0²,⁷]pentadeca-1(15),2(7),5,11,13-pentaen-6-yl}pyrrolidin-3-amine dihydrochloride

Smiles: Cl.Cl.N[C@H]1CN(CC1)C1=NC(=N)NC2C3=CC=CC=C3CCCC1=2

InChiKey: ISYUFRNZHUOGLA-CURYUGHLSA-N

InChi: InChI=1S/C17H21N5.2ClH/c18-12-8-9-22(10-12)16-14-7-3-5-11-4-1-2-6-13(11)15(14)20-17(19)21-16;;/h1-2,4,6,12H,3,5,7-10,18H2,(H2,19,20,21);2*1H/t12-;;/m1../s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.