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2070015-10-8

中文名稱 ML204 HYDROCHLORIDE
英文名稱 ML 204
CAS 2070015-10-8
分子式 C15H19ClN2
分子量 262.78
MOL 文件 2070015-10-8.mol
2070015-10-8 結(jié)構(gòu)式 2070015-10-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T24481
4-甲基-2-(哌啶-1-基)喹啉鹽酸鹽
英文別名
ML204 hydrochloride,ML-204 hydrochloride

物理化學(xué)性質(zhì)

儲(chǔ)存條件Inert atmosphere,2-8°C
形態(tài)Solid
顏色White to off-white

常見(jiàn)問(wèn)題列表

生物活性
ML204 hydrochloride 是一個(gè)有效的、選擇性的 TRPC4/TRPC5 通道的抑制劑,較 TRPC6 的選擇性高出 20 倍,不影響其他的 TRP 通道和電壓門(mén)控的鈉、鉀或 Ca2+ 通道。
靶點(diǎn)

TRPC4

TRPC5

體外研究

ML204 hydrochloride inhibits TRPC4β-mediated intracellular Ca 2+ rise with an IC 50 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 M 2 muscarinic receptors or G q/11 stimulation by the endogenous M 3 -like muscarinic receptors.
ML204 hydrochloride blocks LPS-induced TRPC5 channel activity.

體內(nèi)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.

Animal Model: Nonfasted male C57BL/6 (2-3 months)
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.
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