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HBK001

Chemical Structure : HBK001

CAS No.: 1942922-78-2

HBK001 (HBK 001, HBK-001)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 586.70
Formula C30H38N10O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
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

References

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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