NF449 octasodium
目录号 : KM10649 CAS No. : 627034-85-9 纯度 : 98%

NF449 octasodium 是一种高效的 P2X1 受体拮抗剂,对 rP2X1、rP2X1+5、P2X2+3 的 IC50 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。

规格 价格 是否有货 数量
1mg
In-stock

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生物活性

NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. 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.

体外研究

NF449 suppressed the rate of GTP[γS] binding to rGsα-s while 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).

体内研究

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.

分子式
C41H24N6Na8O29S8
分子量
1505.09
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)

溶解性数据
In Vitro: 

DMSO : 10 mg/mL (6.64 mM; ultrasonic and warming and heat to 60°C)

H2O : 10 mg/mL (6.64 mM; Need ultrasonic and warming

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                   
1 mM 0.6644 mL 3.3221 mL 6.6441 mL
5 mM 0.1329 mL 0.6644 mL 1.3288 mL
10 mM --- --- ---
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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