NF449 octasodium - CAS:627034-85-9

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NF449 octasodium

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

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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 Gs_α 选择性 G 蛋白 (G Protein) 拮抗剂。NF449 octasodium 抑制 GTP[γS] 与 G_sα-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 G_s 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_sα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to G_sα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to G_s.
体外研究	NF449 suppressed the rate of GTP[γS] binding to rG_sα-s while barely affecting binding to rG_iα-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 G_s (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	C₄₁H₂₄N₆O₂₉S₈-₈^.₈[Na+]
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)