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首页-小分子抑制剂&激动剂-GPCR-GPR119-HBK001
HBK001

Chemical Structure : HBK001

CAS No.: 1942922-78-2

HBK001 (HBK 001, HBK-001)

货号: PC-20431Not For Human Use, Lab Use Only.

HBK001 (HBK-001) is a dual-target DPP4 inhibitor and GPR119 agonist with IC50 of 66 nM for DPP4 and EC50 of 30 nM for GPR119 transactivation activity.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

HBK001 (HBK-001) is a dual-target DPP4 inhibitor and GPR119 agonist with IC50 of 66 nM for DPP4 and EC50 of 30 nM for GPR119 transactivation activity.
HBK001 displays no effect on GPR40, GLP1R and GIPR at 10 uM.
HBK001 selectively inhibits DPP4 ex vivo and in vivo.
HBK001 activates GPR119 and induces insulin secretion ex vivo and incretins release in vivo.
HBK001 treatment increased cytosolic cAMP in a concentration-dependent manner in the mouse pancreatic β-cell line NIT-1.
HBK001 (30 mg/kg) improveed glucose tolerance in ICR mice, and ameliorated hyperglycemia in diabetic db/db mice and KKAy mice.
HBK001 promoted insulin secretion and improved islet β-cell function in KKAy mice via a GPR119-dependent pathway.

物理化学性质&存储条件

分子量 586.70
分子式 C30H38N10O3
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

(R)-8-(3-aminopiperidin-1-yl)-7-(but-2-yn-1-yl)-3-methyl-1-(3-(4-(3-phenyl-1,2,4-oxadiazol-5-yl)piperazin-1-yl)propyl)-1H-purine-2,6 (3H, 7H)-dione

参考文献

1. Huan Y, et al. Sci Rep. 2017 Jun 28;7(1):4351.

2. Li G, et al. Eur J Med Chem. 2020 Feb 15;188:112017.

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