13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mg 50mg |
| CAS | 1227675-50-4 |
| 別名 |
|
| 化學名 | (R)-1-(2-imino-2,5,6,7-tetrahydro-1H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-4-yl)pyrrolidin-3-amine dihydrochloride |
| 分子式 | C17H21N5.2HCl |
| 分子量 | 368.31 |
| 溶解度 | <36.83mg/ml in H2O; <36.83mg/ml in DMSO |
| 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 |
產品描述：
A 943931, is an H4R (one of histamine receptor subtypes) antagonist [1] with high affinities to H4Rs of human (Ki = 5 nM), rat (Ki = 4 nM) and mouse (Kb = 6 nM) [2].
H4R is one of 4 known G-protein-coupled receptors (H1, H2, H3 and H4 receptors) of histamine for histamine to mediate its physiological functions [3].
HMC-1 cells incubated with A 943931 at a concentration of 300 nM for 20 min inhibited the increase in ALDH2 activity induced by H4R [4]. In microglia, A 943931 at a concentration of 10 μM partially abolish the release of TNF-α and IL-6 induced by histamine at a concentration of 0.1 μg/ml [5]. In bone marrow-derived mast cells, A 943931 inhibited the shape change induced by histamine (IC50 = 0.38 μM) [6].
Intraperitoneal administration of A 943931 at a dose of 33 μmol/kg potently inhibited itch induced by H4R agonist in mice [6]. In several preclinical models, H4R had been shown to be linked to inflammation [7]. A 943931 had excellent antagonistic activity both in vivo and in vitro across multiple species, displayed good oral bioavailability (90%) and excellent metabolic stability. This compound displays good efficacy in rat pain models and is a good anti-inflammatory agent in mice [8]. A 943931 has an in vivo oral bioavailability of 34% and a half-life of 2.6 h in rats [2]. A 943931 efficaciously reduced acute inflammatory pains induced by formalin in the flinch model and by carrageenan in mechanical and thermal hyperalgesia models in rats [9].
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1. 本產品僅供科研使用。請勿用于醫藥、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。
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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