| Bioactivity | A-943931 is a potent and selective histamine H4 receptor (H4R) antagonist with pKi values of 4.6, 3.8 nM for human and rat H4R, respectively. A-943931 shows anti-inflammatory and antinociceptive efficacy[1][2]. |
| In Vivo | A-943931 在酵母聚糖诱导的小鼠腹膜炎中表现出抗炎活性，皮下注射和腹腔注射的ED50 值分别为 34, 33 µmol/kg[2]。A-943931 (10, 30, 100 µmol/kg; 腹腔注射) 在大鼠的炎症性疼痛和神经性疼痛模型中表现出镇痛效果[2]。 Animal Model: |
| Name | A-943931 |
| CAS | 1027330-97-7 |
| Formula | C17H21N5 |
| Molar Mass | 295.38 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ivan Milicic, et al. Identification of two potent and selective histamine H4 receptor antagonists with antipruritic activity. The FASEB journal homepage. 2009. [2]. Cowart MD, et al. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem. 2008 Oct 23;51(20):6547-57. |