Anagliptin_product_DataBase

Bioactivity

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].

Invitro

Anagliptin (SK-0403) (0-100 μM; 24 h) attenuates s-DPP-4-induced smooth muscle cells proliferation[2].Anagliptin (100 μM; 10 min) reduces TNF-α production in cultured monocytes[2].Anagliptin (0.001-10 μM; 24 h) significantly suppresses sterol regulatory element‐binding protein activity in HepG2 cells (21% decrease)[3]. Cell Proliferation Assay[2] Cell Line:

In Vivo

Anagliptin (SK-0403) (0.3%; in diet; 16 weeks) reduces atherosclerotic lesion and does not increase the number of circulating EPCs in apoliporotein E (apoE)-deficient mice[2].Anagliptin (0.3%; in diet; 4 weeks) exhibits a lipid‐lowering effect in a hyperlipidemic mice model[3]. Animal Model:

Name

Anagliptin

CAS

739366-20-2

Formula

C19H25N7O2

Molar Mass

383.45

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

Anagliptin

CAS: 739366-20-2 F: C19H25N7O2 W: 383.45