CSN19023

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:

1. 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.
2. Miller MR, et al. Novel Chemical Inhibitor of TRPC4 Channels. Probe Reports from the NIH Molecular Libraries Program.
3. Thomas Schaldecker, et al. Inhibition of the TRPC5 ion channel protects the kidney filter. J Clin Invest. 2013 Dec 2; 123(12): 5298–5309.
4. 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.