Anagliptin

Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively[1].

Product Specifications

CAS Number

[739366-20-2]

Product Name Alternative

SK-0403

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Dipeptidyl Peptidase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Anagliptin.html

Concentration

10mM

Purity

99.92

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[C@H](C#N)CCC3)=O)C

Molecular Formula

C19H25N7O2

Molecular Weight

383.45

Precautions

H315, H319, H335

References & Citations

[1]Kato N, et al. Discovery and pharmacological characterization of N-[2- ({2-[ (2S) -2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino) -2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor. Bioorg Med Chem. 2011 Dec 1;19 (23) :7221-7.|[2]Ervinna N, et al. Anagliptin, a DPP-4 inhibitor, suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction and attenuates atherosclerosis in male apo E-deficient mice. Endocrinology. 2013 Mar;154 (3) :1260-70.|[3]Yano W, et al. Mechanism of lipid-lowering action of the dipeptidyl peptidase-4 inhibitor, anagliptin, in low-density lipoprotein receptor-deficient mice. J Diabetes Investig. 2017 Mar;8 (2) :155-160.