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NF449 octasodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NF449 octasodium图片
CAS NO:627034-85-9
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
NF449 octasodium 是一种高效的P2X1受体拮抗剂,对 rP2X1、rP2X1+5、P2X2+3IC50分别为 0.28、0.69 和 120 nM。NF449 octasodium 是一种 Gsα选择性 G 蛋白 (G Protein) 拮抗剂。NF449 octasodium 抑制 GTP[γS] 与 Gsα-s结合的速率,抑制腺苷酸环化酶活性的刺激,阻断 β-肾上腺素能受体与 Gs的偶联。
生物活性

NF449 octasodium is a highly potentP2X1receptorantagonist, withIC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selectiveG Proteinantagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs[1][2].

体外研究
(In Vitro)

NF449 suppressed the rate of GTP[γS] binding to rGsα-swhile barely affecting binding to rGiα-1(IC50=140 nM), inhibits stimulation of adenylyl cyclase activity in S49 cyc– membranes (deficient in endogenous Gsα) by exogenously added Gsα-s, and blocks the coupling of β-adrenergic receptors to Gs(EC50=7.9 μM)[2].

体内研究
(In Vivo)

At a dose of 10 mg/kg, NF449 inhibits the ex vivo aggregation triggered by 5 g/ml collagen in WT mouse platelets without affecting that induced by 5 μM ADP. At a higher dose (50 mg/kg), NF449 inhibits ex vivo platelet aggregation in response to not only 10 g/ml collagen but also 5 M ADP, indicating nonselective inhibition of the P2Y1 and/or P2Y12 receptor[3].

分子量

1505.09

性状

Solid

Formula

C41H24N6Na8O29S8

CAS 号

627034-85-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)