SNX-482 

SNX-482, a peptide, is a potent, high affinity, selective and voltage-dependent R-type Ca_V2.3 channel blocker with an IC₅₀ of 30 nM. SNX-482 has antinociceptive effect^[1][2][3].

IC50: 30 nM (CaV2.3 channel)^[2]

SNX-482 阻断 E 类 Ca²⁺ 通道，IC₅₀ 为 15-30 nM，通过膜片钳电生理学或 K⁺ 诱发的 Ca²⁺ 通量检测^[1]。
在低纳摩尔浓度下，SNX-482 还会阻断大鼠神经垂体神经末梢中的天然抗性或 R 型 Ca²⁺ 电流，但 200-500 nM 的浓度对几种大鼠中枢神经元中的 R 型 Ca²⁺ 电流没有影响^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SNX-482 (0.5-4 μg/50 μL；鞘内给药；术后 14-17 天) 在脊髓神经结扎 (SNL) 的大鼠模型中，剂量依赖性地抑制了伤害性 C 纤维和 Aδ 纤维介导的神经元反应，且对非伤害性机械和热刺激的反应在 SNL 大鼠中比在假手术大鼠中更敏感^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

4495.00

C₁₉₂H₂₇₄N₅₂O₆₀S₇

203460-30-4

固体

White to off-white

Gly-Val-Asp-Lys-Ala-Gly-Cys-Arg-Tyr-Met-Phe-Gly-Gly-Cys-Ser-Val-Asn-Asp-Asp-Cys-Cys-Pro-Arg-Leu-Gly-Cys-His-Ser-Leu-Phe-Ser-Tyr-Cys-Ala-Trp-Asp-Leu-Thr-Phe-Ser-Asp (Disulfide bridge:Cys7-Cys21;Cys14-Cys26;Cys20-Cys33)

GVDKAGCRYMFGGCSVNDDCCPRLGCHSLFSYCAWDLTFSD (Disulfide bridge:Cys7-Cys21;Cys14-Cys26;Cys20-Cys33)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. R Newcomb, et al. Selective peptide antagonist of the class E calcium channel from the venom of the tarantula Hysterocrates gigas. Biochemistry. 1998 Nov 3;37(44):15353-62.  [Content Brief]

  [2]. E Bourinet, et al. Interaction of SNX482 with domains III and IV inhibits activation gating of alpha(1E) (Ca(V)2.3) calcium channels. Biophys J. 2001 Jul;81(1):79-88.  [Content Brief]

  [3]. Elizabeth A Matthews, et al. The Cav2.3 calcium channel antagonist SNX-482 reduces dorsal horn neuronal responses in a rat model of chronic neuropathic pain. Eur J Neurosci. 2007 Jun;25(12):3561-9.  [Content Brief]