NF 449

NF 449

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  • ¥600 - 3200
  • 上海莼试
  • CS-01Y74899
  • 国产
  • 2025年07月14日
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    • 详细信息
    • 技术资料
    • 库存

      40

    • 英文名

      NF 449

    • CAS号

      627034-85-9

    • 供应商

      上海莼试

    • 保存条件

      Store at -20°C

    • 规格

      1mg 5mg 10mg 50mg

    商品属性:
    货号CS-01Y74899规格1mg 5mg 10mg 50mg
    CAS号627034-85-9分子量1505.06
    含量>95.00%别名N/A
    分子式C41H24N6Na8O29S8化学名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
    产地国产用途仅供科研研究实验
    产品描述:
    分子式:C41H24N6Na8O29S8

    NF 449
    分子量:1505.06
    溶解度:PBS (pH 7.2): 10 mg/ml
    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                                      
    IC50: 0.28 nm for rP2X1NF 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 orvations 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.
    注意事项:
    抗逆滴加序列
    每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
    抗感染反应期
    抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
    旅游温度
    磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
    当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
    反应时间及温度
    加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
    使用方法:
    1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
    2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。
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