13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
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 | 1mg 5mg 10mg 50mg |
| CAS | 627034-85-9 |
| 別名 | N/A |
| 化學名 | sodium (1Z,3Z)-5-(((Z)-((3,5-bis((Z)-oxido((2-sulfo-4-sulfonatophenyl)imino)methyl)phenyl)imino)oxidomethyl)amino)-N'1-(2,4-disulfophenyl)-N'3-(2-sulfo-4-sulfonatophenyl)isophthalimidate |
| 分子式 | C41H24N6Na8O29S8 |
| 分子量 | 1505.06 |
| 溶解度 | PBS (pH 7.2): 10 mg/ml |
| 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：
IC50: 0.28 nm for rP2X1
NF 449 is a potent purinergic receptor antagonist that displays high selectivity for P2X1. The P2X1 ion channel is activated by ATP among the three P2 receptor subtypes present on blood platelets.
In vitro: The interaction of the A1-adenosine receptor with its cognate G proteins (Gi/Go) disrupted by NF503 and NF449 at concentrations that are >30- fold higher than those required for uncoupling of b-adrenergic receptor/Gs tandems; similarly, the compounds barely affected the angiotensin II type-1 receptor . Thus, NF503 and NF449 achieve essential criteria for Gsa-selective antagonists. The observations demonstrate that subtype-selective G protein inhibition is feasible[1]. inhibited 5-triphosphate-induced shape change in treatment of washed human platelets with apyrase to abolish desensitization of the P2X1 receptor. The calcium rise mediated by the P2Y1 receptor was also antagonized by NF449, but with lower potency. In contrast, NF449 was a very weak antagonist of inhibiting adenylyl cyclase activity mediated by P2Y12. Selective blockade of the P2X1 receptor with NF449 led to decreased collagen-induced aggregation. Therefore, a role of this receptor in platelet activation induced by collagen was confirmed [2]. So far, characterize NF449 as the most potent and selective antagonist of receptors (the P2X1 subunit such as the P2X1 homomer and the P2X1C5 heteromer) [3].
In vivo: Intravenous injection of 10 mg/kg NF449 into mice exhibited selective inhibition of the P2X1 receptor and reduced intravascular platelet aggregation in a model of systemic thromboembolism without prolongation of the bleeding time. At a higher dose (50 mg/kg), NF449 blocked the three platelet P2 receptors. This, compared with mice injected with saline, led to a further reduction in platelet consumption. NF449 also decreased dose-dependently the size of thrombi formed after laser-induced injury of mesenteric arterioles. Overall, our results indicate that NF449 constitutes a new agent to investigate the functions of the P2X1 receptor and could be a starting compound in the investigation for new antithrombotic drugs targeting the platelet tP2 receptors [2].
Clinical trial: So far, no clinical study has been conducted.
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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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