ML204

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 Chemical Structure

ML204 Chemical Structure

CAS: 5465-86-1

Selleck's ML204 has been cited by 1 publication

Purity & Quality Control

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

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Biological Activity

Description 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.
Targets
TRPC4 [1]
In vitro
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. ML204 block of TRPC4β channels is not dependent upon GPCR activation. Selectivity studies show no appreciable block by 10-20 μM ML204 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. 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].
Cell Research Cell lines HEK293 cells
Concentrations 10 μM
Incubation Time --
Method

--

Chemical Information & Solubility

Molecular Weight 226.32 Formula

C15H18N2

CAS No. 5465-86-1 SDF Download ML204 SDF
Smiles CC1=CC(=NC2=CC=CC=C12)N3CCCCC3
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 45 mg/mL ( (198.83 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 45 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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