ML204

製品コードS8691 バッチS869101

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₅H₁₈N₂

分子量

226.32

CAS No.

5465-86-1

Solubility (25°C)*

体外

DMSO

45 mg/mL (198.83 mM)

Ethanol

45 mg/mL (198.83 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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 G_i/o stimulation by μ-opioid, 5HT1A serotonin, and M2 muscarinic receptors or G_q/11 stimulation by the endogenous M3-like muscarinic receptors^[1].

製品説明

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.

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 G_i/o stimulation by μ-opioid, 5HT1A serotonin, and M2 muscarinic receptors or G_q/11 stimulation by the endogenous M3-like muscarinic receptors^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK293 cells
	濃度	10 μM
	反応時間	--
	実験の流れ	--

参考

https://pubmed.ncbi.nlm.nih.gov/21795696/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Autophagy induction via STING trafficking is a primordial function of the cGAS pathway [Gui X, et al Nature, 2019, 567(7747):262-266]	PubMed: 30842662

Autophagy induction via STING trafficking is a primordial function of the cGAS pathway [Gui X, et al Nature, 2019, 567(7747):262-266]

PubMed: 30842662

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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