PSB-172656 | MRGPRX2 antagonist | Probechem Biochemicals

Chemical Structure : PSB-172656

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PSB-172656 (PSB172656)

货号: PC-24413Not For Human Use, Lab Use Only.

PSB-172656 is a highly potent, selective non-cytotoxic MAS-related G protein-coupled receptor-X2 (MRGPRX2) antagonist with Ki of 0.142 nM, does not block any of the other MRGPRX subtypes at 10 uM.

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生物&药学活性

PSB-172656 is a highly potent, selective non-cytotoxic MAS-related G protein-coupled receptor-X2 (MRGPRX2) antagonist with Ki of 0.142 nM, does not block any of the other MRGPRX subtypes at 10 uM.
PSB-172656 not only inhibited MRGPRX2 activation induced by the peptide CST-14 (Ki 6.81nM), but also by all other investigated agonists including the peptide substance P (SP; Ki 8.82 nM.
PSB-172656 (100 nM) completely inhibited MRGPRX2-induced Gαq as well as Gαi1 protein activation.
PSB-172656 (100 nM, 300 nM) inhibits MRGPRX2-mediated MC activation utilizing the rat MC line RBL-2H3 recombinantly expressing the human MRGPRX2, completely abolished MC degranulation in response to C48/80 and SP, inhibited degranulation in response to all of the investigated MRGPRX2 agonists in a concentration-dependent manner with similarly high IC50 values: C48/80 (3.79 nM), SP (15.5 nM), PAMP-12 (11.7nM), and LL-37 (8.12 nM).
PSB-172656 inhibited MRGPRX2-mediated Ca2+ mobilization in LAD2 cells, caused a dose-dependent inhibition of β-hexosaminidase release in LAD2 cells in response to SP with IC50 of 5.26 nM in recombinant RBL-MRGPRX2 MC line.
PSB-172656 additionally blocks the putative mouse ortholog of MRGPRX2, MRGPRB2, as determined in Ca2+ mobilization assays (Ki 0.302 nM).
PSB-172656 prevents mouse tracheal contractions, local allergic reactions, and systemic anaphylactic symptoms.

物理化学性质&存储条件

分子量	291.30
分子式	C15H15F2N3O
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-ethyl-7,8-difluoro-2-isopropylbenzo[4,5]imidazo [1,2-a] pyrimidin-4(1H)-one

参考文献

1. Al Hamwi G, et al. Signal Transduct Target Ther. 2025 Apr 21;10(1):128.

PSB-172656 (PSB172656)

生物&药学活性

物理化学性质&存储条件

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PSB-172656 (PSB172656)

生物&药学活性

物理化学性质&存储条件

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