ML 204

CAS No.2070015-10-8
Chemical Name:ML 204
CBNumber:CB23373068
Molecular Formula:C15H19ClN2
Formula Weight:262.78
MOL File:2070015-10-8.mol

storage temp. under inert gas (nitrogen or Argon) at 2-8°C
form Solid
color White to off-white

Symbol(GHS)
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Hazard statements
Precautionary statements

Uses 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 Ca2+ channels[1][2].
Biological Activity ML204 is a potent and selective inhibitor of TRPC4/TRPC5 channels with 20-fold selectivity over TRPC6, without affecting other TRP channels and voltage-gated sodium, potassium or Ca2+ channels.
in vitro

ML204 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.
It 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.
It blocks LPS-induced TRPC5 channel activity.
in vivo

ML204 (1 mg/kg; sc; twice a day; for 5 days) causes mortality associated with exacerbated hypothermia and decreases peritoneal leukocyte numbers and cytokines in LPS-injected mice.

< td class="col2"> Subcutaneous injection, twice a day, for 5 days (prior to LPS injection) < td class="col2"> Induces mortality associated with increased hypothermia in mice with LPS-induced systemic inflammatory response.

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

Dosage: 1 mg/kg

Administration:

Result:

target

IC 50 TRPC4; TRPC5

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. DOI:10.1074/jbc.M111.274167
[2] Miller MR, et al. Novel Chemical Inhibitor of TRPC4 Channels. Probe Reports from the NIH Molecular Libraries Program. PMID:22049577
[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. DOI:10.1172/JCI71165
[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. DOI:10.1155/2018/4904696

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