| Bioactivity | A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model[1]. |
| Invitro | A-987306 has potent functional antagonism in vitro at human, rat, and mouse H4 receptors in cell-based FLIPR assays[1].A-987306 is 620-fold, >1600-fold, and 162-fold selective for the human H4R over the human H1, H2 , and H3 receptors in cell-based Ca2+-flux functional assay (FLIPR)[1].A-987306 shows lower selectivity for H4R in the rat (only 4-fold selective for the rat H4R over the rat H3R) in FLIPR[1]. |
| In Vivo | A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) is found to reduce scratching induced by the histamine H4 agonist clobenpropit (HY-101198)[1].A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (Fpo/iv=26%) with a half-life of 3.7 h and a Cmax of 0.30 µM at a Tmax of 1.5 h after dosing[1]. Animal Model: |
| Name | A-987306 |
| CAS | 1082954-71-9 |
| Formula | C18H25N5O |
| Molar Mass | 327.42 |
| 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]. cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia J. Med. Chem., 2008, 51 (22), pp 7094-7098 |