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首页-小分子抑制剂&激动剂-GPCR-Bradykinin Receptor-Deucrictibant
Deucrictibant

Chemical Structure : Deucrictibant

CAS No.: 2340111-58-0

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Deucrictibant (PHA121, PHA-022121)

货号: PC-26637Not For Human Use, Lab Use Only.

Deucrictibant (PHA-022121, PHA121) is a potent, selective and oral bradykinin B2 receptor (B2R) antagonist with Ki of 0.47 nM for recombinant human bradykinin B2 receptor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Deucrictibant (PHA-022121, PHA121) is a potent, selective and oral bradykinin B2 receptor (B2R) antagonist with Ki of 0.47 nM for recombinant human bradykinin B2 receptor.
Deucrictibant (PHA-022121, PHA121) exhibits potent antagonism of human bradykinin B2 receptor with Kb value of 0.15 nM (calcium mobilization assay).
Deucrictibant (PHA-022121, PHA121) shows similar antagonist potency at the recombinant cynomolgus monkey bradykinin B2 receptor.
Deucrictibant (PHA-022121, PHA121) shows a potent, surmountable and reversible B2 antagonist activity with pA2 value of 0.35 nM in human umbilical vein contractility assay.

物理化学性质&存储条件

分子量 534.94
分子式 C25H22DClF3N5O3
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

Acetamide, N-[(1S)-1-[3-chloro-5-fluoro-2-[[[2-methyl-4-(1-methyl-1H-1,2,4-triazol-5-yl)-8-quinolinyl]oxy]methyl]phenyl]ethyl-1-d]-2-(difluoromethoxy)-

参考文献

1. Petersen RS, et al. J Allergy Clin Immunol. 2024 Jul;154(1):179-183.

2. Aygören-Pürsün E, et al. Lancet Haematol. 2026 Apr;13(4):e215-e226.

3. Lesage A, et al. Int Immunopharmacol. 2022 Apr;105:108523.

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