Description
ML204 HCl is a potent, selective TRPC4 channel inhibitor with IC50 of 0.96 μM.
Product information
CAS Number: 2070015-10-8
Molecular Weight: 262.78
Formula: C15H19ClN2
Chemical Name: 4-Methyl-2-(1-piperidinyl)quinoline hydrochloride
Smiles: Cl.CC1=CC(=NC2=CC=CC=C21)N1CCCCC1
InChiKey: QCABWRXQHZUBPW-UHFFFAOYSA-N
InChi: InChI=1S/C15H18N2.ClH/c1-12-11-15(17-9-5-2-6-10-17)16-14-8-4-3-7-13(12)14;/h3-4,7-8,11H,2,5-6,9-10H2,1H3;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: H2O : ≥ 30 mg/mL (114.16 mM)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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 Gi/o stimulation by μ-opioid, 5HT1A serotonin, and M2 muscarinic receptors or Gq/11 stimulation by the endogenous M3-like muscarinic receptors. ML204 hydrochloride blocks LPS-induced TRPC5 channel activity.
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.
References:
- Miller M, et al. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46.
- Miller MR, et al. Novel Chemical Inhibitor of TRPC4 Channels. Probe Reports from the NIH Molecular Libraries Program.
- Thomas Schaldecker, et al. Inhibition of the TRPC5 ion channel protects the kidney filter. J Clin Invest. 2013 Dec 2; 123(12): 5298–5309.
- Domingos M S Pereira, et al. Transient Receptor Potential Canonical Channels 4 and 5 Mediate Escherichia coli-Derived Thioredoxin Effects in Lipopolysaccharide-Injected Mice. Oxid Med Cell Longev. 2018 Jun 10;2018:4904696.
Products are for research use only. Not for human use.
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