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首页-小分子抑制剂&激动剂-GPCR-Mas-related G protein-coupled receptor (MRGPR)-MS47134
MS47134

Chemical Structure : MS47134

CAS No.:

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MS47134 (MS 47134)

货号: PC-38069Not For Human Use, Lab Use Only.

MS47134 is a potent, selective MRGPRX4 agonist with EC50 of 149 nM.

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

生物&药学活性

MS47134 is a potent, selective MRGPRX4 agonist with EC50 of 149 nM.
MS47134 displays 47-fold improved selectivity for MRGPRX4 over the Kir6.2/SUR1 potassium channel.
Off-target profiling of MS47134 at 320 GPCRs showed activity only at MRGPRX4 and MRG-PRX1 with no appreciable agonist or antagonist activity at the other 318 tested GPCRs.
MS47134 binds to MRGP RX4 on the extrac ellular side far from t he canonical to ggle switch W6.48 in 5-HT2AR.
A Y130ICL2A mutation reduced the agonist potency of MS47134 while the Y137ICL2A mutation in MRG-PRX2 has little effect.

物理化学性质&存储条件

分子量 355.478
分子式 C22H29NO3
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

10 mM in DMSO
Chemical Name/SMILES

(3,5-dimethyladamantane-1-carbonyl)-D-phenylalanine

参考文献

1. Can Cao, et al. Nature. 2021 Dec;600(7887):170-175.

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