Anagliptin

Anagliptin is a highly selective, potent inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8/9 (IC50, 68, 60 nM, respectively).

Product information

CAS Number: 739366-20-2

Molecular Weight: 383.45

Formula: C19H25N7O2

Chemical Name: N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide

Smiles: CC1C=C2N=CC(=CN2N=1)C(=O)NCC(C)(C)NCC(=O)N1CCC[C@H]1C#N

InChiKey: LDXYBEHACFJIEL-HNNXBMFYSA-N

InChi: InChI=1S/C19H25N7O2/c1-13-7-16-21-9-14(11-26(16)24-13)18(28)22-12-19(2,3)23-10-17(27)25-6-4-5-15(25)8-20/h7,9,11,15,23H,4-6,10,12H2,1-3H3,(H,22,28)/t15-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (260.79 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Anagliptin is a highly selective, potent inhibitor of DPP-IV, with an IC50 of 3.8 nM, and less selective at DPP-8/9 (68, 60 nM, respectively). Anagliptin does not affect CYP3A4, CYP2C19, CYP2C9, CYP1A2, and CYP2D6 (IC50 >10 μM) or CYP3A4, CYP2C8, CYP2C9, and CYP1A2 at 50 μM. Anagliptin hydrochloride does not bind to the hERG channel (E-4031, >90% inhibition at 0.1 μM, IC50 >500 μM in patch clamp using HEK 293 cells). Anagliptin (1-100 μM) dose-dependently suppresses-DPP-4-induced smooth muscle cells (SMCs) proliferation, and reduces TNF-α production in cultured monocytes.

In Vivo:

Anagliptin (0.3%) alters the quantity and quality of atherosclerotic lesions in apoE-deficient mice, and reduces DPP-4 activity in the plasma, and total cholesterol level, especially VLDL and LDL-C in mice. Anagliptin also decreases α-SMA-positive area and TNF-α-positive lesions in plaque area of apoE-deficient mice. In addition, Anagliptin does not increase the number of circulating endothelial progenitor cells (EPCs) in apoE-deficient mice. Anagliptin (0.3%) decreases the low-density lipoprotein cholesterol and very low-density lipoprotein cholesterol, and also reduces the sterol regulatory element-binding protein-2 messenger ribonucleic acid expression level in mice.

Products are for research use only. Not for human use.