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ML204 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML204 hydrochloride图片
CAS NO:2070015-10-8
包装与价格:
包装价格(元)
10 mM * 1 mL in Water电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

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, selectiveTRPC4/TRPC5channel 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[1][2].

IC50& Target[1][2]

TRPC4

 

TRPC5

 

体外研究
(In Vitro)

ML204 hydrochloride inhibits TRPC4β-mediated intracellular Ca2+rise with an IC50value of 0.96 μM (HEK293 cells) and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation[1].
ML204 hydrochloride blocks TRPC4β activity induced through either Gi/ostimulation by μ-opioid, 5HT1Aserotonin, and M2muscarinic receptors or Gq/11stimulation by the endogenous M3-like muscarinic receptors[1].
ML204 hydrochloride blocks LPS-induced TRPC5 channel activity[3].

体内研究
(In Vivo)

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].

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.
分子量

262.78

性状

Solid

Formula

C15H19ClN2

CAS 号

2070015-10-8

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)

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 mg5 mg10 mg
1 mM3.8055 mL19.0273 mL38.0546 mL
5 mM0.7611 mL3.8055 mL7.6109 mL
10 mM0.3805 mL1.9027 mL3.8055 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。