Anagliptin (SK-0403) 是一种高选择性的、有效的、具有口服活性的二肽酰肽酶 4 (DPP-4) 抑制剂，IC₅₀ 值为 3.8 nM，对 DPP-8 和 DDP-9 的选择性相对较弱，IC₅₀ 值分别为 68 nM 和 60 nM。

Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC 50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC 50 s of 68 nM and 60 nM, respectively.

Solid

DPP-4 3.8 nM (IC50) DPP-9 60 nM (IC5

Anagliptin (SK-0403) (0-100 μM; 24 h) attenuates s-DPP-4-induced smooth muscle cells proliferation.
Anagliptin (100 μM; 10 min) reduces TNF-α production in cultured monocytes.
Anagliptin (0.001-10 μM; 24 h) significantly suppresses sterol regulatory element‐binding protein activity in HepG2 cells (21% decrease). has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay

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.
Anagliptin (0.3%; in diet; 4 weeks) exhibits a lipid‐lowering effect in a hyperlipidemic mice model. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (260.79 mM; Need ultrasonic)配制储备液