| Bioactivity | ML204 is a 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]. | ||||||||||||
| Invitro | ML204 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[1].ML204 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[1].ML204 blocks LPS-induced TRPC5 channel activity[3]. | ||||||||||||
| In Vivo | ML204 (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[4]. Animal Model: | ||||||||||||
| Name | ML204 | ||||||||||||
| CAS | 5465-86-1 | ||||||||||||
| Formula | C15H18N2 | ||||||||||||
| Molar Mass | 226.32 | ||||||||||||
| Appearance | Oil | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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 [Internet]. [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. |