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 Ca 2+ channels In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:TRPC4|TRPC5
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ML204 hydrochloride
CAS number：2070015-10-8 molecular formula：C15H19ClN2
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| Chinese alias | ML204 盐酸盐 | ||
| English alias | 4-Methyl-2-(piperidin-1-yl)quinoline hydrochloride | ML204 HCl | AKOS032945007 | ML204 hydrochloride | ML 204 HCl; ML204 hydrochloride; ML 204 hydrochloride; ML-204 hydrochloride | MLS003227299 | BS-15926 | HY-12949A | ML204hydrochloride | 4-methyl-2-pipe | ||
| CAS number | 2070015-10-8 | molecular formula | C15H19ClN2 |
| molecular weight | 262.78 g/mol | Exact mass | ≥99% |
| PSA | 16.100 Ų | logp | - |
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