2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. BTT-369

BTT-369 是一种 CaVα1·CaVβ3 蛋白-蛋白复合物拮抗剂，其 Ki 为 2.0 μM。BTT-369 抑制 CaV2.2 电流，表观 IC50 值为 31 μM。BTT-369 可破坏 CaVα1-CaVβ3 亚基间的相互作用。BTT-369 可减小 CaV2.2 电流密度，并使 CaV2.2 的稳态失活和激活电压依赖性向更正的电位偏移。BTT-369 可减轻大鼠胫神经损伤模型中的机械性痛觉超敏。BTT-369 可用于神经性疼痛的研究。

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BTT-369

BTT-369 Chemical Structure

CAS No. : 2413939-96-3

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BTT-369 相关抗体

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BTT-369 is a CaVα1·CaVβ3 protein-protein complex antagonist with a Ki of 2.0 μM. BTT-369 inhibits CaV2.2 currents, with an apparent IC50 value of 31 μM. BTT-369 disrupts the interaction between CaVα1 and CaVβ3 subunits. BTT-369 reduces the current density of CaV2.2, and shifts the voltage dependence of steady-state inactivation and activation of CaV2.2 to more positive potentials. BTT-369 alleviates mechanical hyperalgesia in a rat model of tibial nerve injury. BTT-369 can be used for the study of neuropathic pain[1].

IC50 & Target[1]

CaV2.2

31 μM (IC50)

体外研究
(In Vitro)

BTT-369 可强效抑制纯化的 CaVα1-AID 与 CaVβ3 之间的蛋白质-蛋白质相互作用，其 Ki 值为 2.0 μM[1]。
BTT-369 (0.1-100 μM；5 min-48 h) 降低 HEK-CaV2.2 细胞中的 CaV2.2 电流密度，将 CaV2.2 激活的电压依赖性和稳态失活的电压依赖性向更正电位方向偏移[1]。

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

BTT-369 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t
Mice[1] 1 mg/kg i.v. 0.29 h 0.083 h 181.36 ng/mL 57.99
Mice[1] 10 mg/kg p.o. 1.99 h 1 h 164.7 ng/mL 635.555
体内研究
(In Vivo)

BTT-369 (0.1 mg/kg；腹腔注射；单次推注) 可在大鼠胫神经损伤神经病理性疼痛模型中显著逆转机械性痛觉超敏[1]。

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

580.64

Formula

C34H28N8O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

BTT-369 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BTT-3692413939-96-3BTT369BTT 369Calcium ChannelCa2+ channelsCa channelsneuropathic painCaVα1-CaVβ3 subunit interactionrat tibial nerve injury modelCaV2.2 channelCaVα1-AIDCaVα1·CaVβ3 protein-protein complexCaVβ3 Arg-307HEK-CaV2.2 cellsInhibitorinhibitorinhibit

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