1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. Calcium Channel Sodium Channel
  3. LY393615

LY393615 (NCC1048) 是一种新型神经元 Ca2+ (calcium channel)和 Na + 通道 (sodium channel) 阻滞剂。LY393615 有良好的脑渗透性,在脑缺血模型中具有神经保护作用。可用于神经性疾病研究。

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LY393615 Chemical Structure

LY393615 Chemical Structure

CAS No. : 325819-97-4

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LY393615 (NCC1048) is a novel neuronal Ca2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research[1].

IC50 & Target

P/Q-type calcium channel

4 μM (IC50)

体外研究
(In Vitro)

LY393615 (0-10 μM) 抑制 HEK293 细胞的钙通量,对 α1A 和 α1B 钙通道亚基的 IC50 分别为 1.9 μM 和 5.2 μM,抑制分离的 Purkinje 细胞中的 P 型钙通道的 IC50 为 4.0 μM[1]

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

体内研究
(In Vivo)

LY393615 (12.5 或 15 mg/kg;腹腔注射, 单次) 保护大脑免受低氧低血糖损伤,并对沙鼠全脑缺血引起的海马损伤提供显着保护[1]。 LY393615 (腹腔注射 15 mg/kg;静脉注射 1 mg/kg) 有具有良好的脑渗透性,T1/2 分别为 2.04 小时 (静脉注射) 和 2.5 小时 (静脉注射) [1] Pharmacokinetic parameters for LY393615 in Gerbils[1]

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

Route Dose (mg/kg) T1/2 (h)
i.v. 1 2.04
i.p. 15 2.5
Animal Model: Gerbils global cerebral ischaemia[1]
Dosage: 10, 12.5 or 15 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Protected against hypoxiahypoglycaemic insults in brain slices and also provided significant protection against ischaemia-induced hippocampal damage in gerbil global cerebral ischaemia.
Animal Model: Gerbils (Pharmacokinetic assay)[1]
Dosage: 1.0 or 15 mg/kg
Administration: Intraperitoneal injection (i.p.) ; Intravenous injection (i.v.)
Result: Had good brain penetration with T1/2s of 2.04 hours (i.v.) and 2.5 hours (i.p.)[1].
分子量

381.89

Formula

C21H26ClF2NO

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
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  • 稀释计算器

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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.

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产品名称:
LY393615
目录号:
HY-135478
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