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ML204 TRP Channel inhibitor

Cat.No.S8691

ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels.
ML204 TRP Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 226.32

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Quality Control

Batch: S869101 DMSO]45 mg/mL]false]Ethanol]45 mg/mL]false]Water]Insoluble]false Purity: 99.93%
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99.93

Solubility

In vitro
Batch:

DMSO : 45 mg/mL (198.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 45 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 226.32 Formula

C15H18N2

 Storage (From the date of receipt)
CAS No. 5465-86-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC(=NC2=CC=CC=C12)N3CCCCC3

Mechanism of Action

Targets/IC50/Ki
TRPC4
In vitro
ML204 inhibits TRPC4β-mediated intracellular Ca2+ rise with an IC50 value of 0.96 μM and exhibits 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. This compound block of TRPC4β channels is not dependent upon GPCR activation. Selectivity studies show no appreciable block by 10-20 μM of this chemical of TRPV1, TRPV3, TRPA1, and TRPM8, as well as KCNQ2 and native voltage-gated sodium, potassium, and calcium channels in mouse dorsal root ganglion neurons. It 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.
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