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首页-小分子抑制剂&激动剂-GPCR-Protease-activated Receptor (PAR)-NRD-21
NRD-21

Chemical Structure : NRD-21

CAS No.: 2403529-11-1

NRD-21 (NRD21, PAR1 NAM NRD-21)

货号: PC-20576Not For Human Use, Lab Use Only.

NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.

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

生物&药学活性

NRD-21 is a potent, selective, reversible, negative allosteric modulator of PAR1 with IC50 of 0.37 uM in calcium mobilization assays.
NRD-21 is a negative allosteric modulator of TFLLRN-NH2 at PAR1, rather than a simple competitive inhibition.
NRD-21 (10 uM) caused complete inhibition of platelet aggregation in human platelets in the presence of the PAR1/2 agonist SFLLRN-NH2 (1.5 μM).
NRD-21 (10 uM) inhibited TNF-α (25 ng/mL) induced TF expression in HUVEC.
NRD-21 shows slightly improved potency over Parmodulin 2 (Cat. PC-62640, ML161, IC50=0.57 uM), but with much improved plasma stability, making it more suitable for in vivo studies.

物理化学性质&存储条件

分子量 386.21
分子式 C17H12BrN3O3
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

N-(3-(2-bromobenzamido)phenyl)oxazole-5-carboxamide

参考文献

1. Disha M Gandhi, et al. Bioorg Med Chem. 2019 Sep 1;27(17):3788-3796.

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