A-943931 is a potent and selective histamine H4 receptor antagonist in functional assays across species (FLIPR Ca (2+) flux, K b < 5.7 nM), has high (>190x) selectivity for H 4, and combines good PK in rats and mice (t 1/2 of 2.6 and 1.6 h, oral bioavailability of 37% and 90%) with anti-inflammatory activity (ED 50 = 37 micromol/kg, mouse) and efficacy in pain models (thermal hyperalgesia, ED 50 = 72 micromol/kg, rat). Blocks inflammation in a peritonitis mouse model and displays efficacy in inflammatory pain and neuropathic pain models. Shows anti-inflammatory and analgesic effects in vivo. Orally active.
MedKoo Cat#: 581019
Name: A-943931 HCl
CAS#: 1227675-50-4 (HCl)
Chemical Formula: C17H23Cl2N5
Exact Mass: 295.1797
Molecular Weight: 368.31
Elemental Analysis: C, 55.44; H, 6.29; Cl, 19.25; N, 19.02
The following data is based on the product molecular weight 368.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
