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+ channelsIn VitroML204 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 VivoML204 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:SolidIC50& Target:TRPC4|TRPC5. Specification: 0.99 Molecular Formula: C15H19ClN2 Molecular Weight: 262.78 PubChem CID: 49786978 Isomeric SMILES: CC1=CC(=NC2=CC=CC=C12)N3CCCCC3.Cl
- UPC:
- 51182107
- Condition:
- New
- Availability:
- 8-12 weeks
- Weight:
- 1.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- M649192-100mg
- CAS:
- 2070015-10-8
- Product Size:
- 100mg
