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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-ML204
ML204

Chemical Structure : ML204

CAS No.: 5465-86-1

ML204 (ML-204)

货号: PC-43288Not For Human Use, Lab Use Only.

ML204 is a potent, selective antagonist of TRPC4 and TRPC5 channels, inhibits TRPC4β-mediated intracellular Ca(2+) rise with IC50 of 0.96 uM, exhibits 19-fold selectivity against TRPC6 channel.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ML204 is a potent, selective antagonist of TRPC4 and TRPC5 channels, inhibits TRPC4β-mediated intracellular Ca(2+) rise with IC50 of 0.96 uM, exhibits 19-fold selectivity against TRPC6 channel.
ML204 blocks TRPC4β currents activated through either μ-opioid receptor stimulation (50 nm DAMGO, IC50=3.55 uM) or intracellular dialysis of GTPγS (IC50=2.85 uM).
ML204 shows no appreciable block by 10-20 uM for TRPV1, TRPV3, TRPA1, and TRPM8, as well as KCNQ2 and Nav Channels.
ML204 also inhibits TRPC5 channel currents activated through co-stimulation of Gi/o and Gq/11 signaling by μ-opioid and M3-like muscarinic receptors.

物理化学性质&存储条件

分子量 226.3168
分子式 C15H18N2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 37 mg/mL

Chemical Name/SMILES

Quinoline, 4-methyl-2-(1-piperidinyl)-

参考文献

1. Miller M, et al. J Biol Chem. 2011 Sep 23;286(38):33436-46.

2. Zhang L, et al. Neuropharmacology. 2013 Sep;72:106-15.

3. Carson C, et al. PLoS One. 2015 Jun 22;10(6):e0127498.

4. Alawi KM, et al. Ann Rheum Dis. 2017 Jan;76(1):252-260.

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