產(chǎn)品目錄

規(guī)格	10mg 50mg
CAS	1082954-71-9
別名
化學名	(7aR,11aR)-4-(piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine
分子式	C18H25N5O
分子量	327.42
溶解度	<32.74mg/ml in DMSO; <32.74mg/ml in ethanol
儲存條件	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

產(chǎn)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].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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