ML204 hydrochloride|cas:2070015-10-8|西域试剂

ML204 hydrochloride,99.81%

产品编号：Bellancom-12949A| CAS NO：2070015-10-8| 分子式：C₁₅H₁₉ClN₂| 分子量：262.78

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货号	价格	库存与货期
Bellancom-12949A	￥770.00	杭州北京（现货）
Bellancom-12949A	￥1200.00	杭州北京（现货）
Bellancom-12949A	￥4200.00	杭州北京（现货）
Bellancom-12949A	￥6200.00	杭州北京（现货）

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ML204 hydrochloride

产品介绍

ML204 hydrochloride 是一个有效的、选择性的 TRPC4/TRPC5 通道的抑制剂，较 TRPC6 的选择性高出 20 倍，不影响其他的 TRP 通道和电压门控的钠、钾或 Ca²⁺ 通道。

生物活性

ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca²⁺ channels.

体外研究

ML204 hydrochloride inhibits TRPC4β-mediated intracellular Ca²⁺ rise with an IC₅₀ value of 0.96 μM (HEK293 cells) and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation.
ML204 hydrochloride blocks TRPC4β activity induced through either G_i/o stimulation by μ-opioid, 5HT_1A serotonin, and M₂ muscarinic receptors or G_q/11 stimulation by the endogenous M₃-like muscarinic receptors.
ML204 hydrochloride blocks LPS-induced TRPC5 channel activity.

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

体内研究

ML204 hydrochloride (1 mg/kg; s.c.; twice a day; for 5 days) causes mortality associated with exacerbated hypothermia and decreases peritoneal leukocyte numbers and cytokines in LPS-injected mice^[4].

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

Animal Model:	Nonfasted male C57BL/6 (2-3 months)^[4]
Dosage:	1 mg/kg
Administration:	Subcutaneous injection, twice a day, for 5 days (prior to LPS injection)
Result:	Induces mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response.

体内研究

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

Animal Model:	Nonfasted male C57BL/6 (2-3 months)^[4]
Dosage:	1 mg/kg
Administration:	Subcutaneous injection, twice a day, for 5 days (prior to LPS injection)
Result:	Induces mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response.

性状

Solid

溶解性数据

In Vitro:

H₂O : ≥ 30 mg/mL (114.16 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.8055 mL	19.0273 mL	38.0546 mL
5 mM	0.7611 mL	3.8055 mL	7.6109 mL
10 mM	0.3805 mL	1.9027 mL	3.8055 mL

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 (sealed storage, away from moisture)。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

参考文献