| CAS NO: | 1082954-71-9 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1082954-71-9 |
| 化学名 | (7aR,11aR)-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine |
| Canonical SMILES | NC(N=C1N2CCNCC2)=NC3=C1CCC4=C3[C@@H](CCCC5)[C@@H]5O4 |
| 分子式 | C18H25N5O |
| 分子量 | 327.42 |
| 溶解度 | <32.74mg/ml in DMSO;<32.74mg/ml in ethanol |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | A987306,cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quin- azolin-2-amine[1], is a selective and potent H4 receptor antagonist [2]. H4R is one of 4 known G-protein-coupled receptors (H1, H2, H3 and H4 receptors) of histamine. It is for mediating some physiological functions of histamine [3]. In a cell-based Ca2+-flux functional assay, A 987306 had no activation to the receptor, but blocked the H4R activation induced by endogenous histamine. A 987306 potently decreased histamine-mediated binding between rat H4-receptor-containing membranes and GTP-γ-[35S] with a Kb of 6 nM [3]. In Sprague-Dawley rats, after ip injection, A 987306 had a favorable fractional bioavailability (Fip/iv =72%), a half-life of 4.7 h and a Cmax of 1.73 μM at a Tmax of 0.25 h after dosing. After oral dosing, A 987306 had 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. The plasma protein binding of A 987306 measured in rats was found to be 59% [3]. To human H4R and rat H4R, the Ki values of A 987306 are 5.8 nM and 3.4 nM, respectively. A 987306 reduced scratch responses in mice with an ED50 of 0.36 μmol/kg. A 987306 was found to be selective and bear an IC50 >810 nM for over 100 kinases [3]. References: |
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