Vincamine

Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.

Product information

CAS Number: 1617-90-9

Molecular Weight: 354.44

Formula: C21H26N2O3

Chemical Name: methyl (15S,17S,19S)-15-ethyl-19-hydrogenio-17-hydroxy-1,11-diazapentacyclo[9.6.2.0²,⁷.0⁸,¹⁸.0¹⁵,¹⁹]nonadeca-2,4,6,8(18)-tetraene-17-carboxylate

Smiles: CC[C@]12C[C@](O)(C(=O)OC)N3C4[C@H]1N(CCC=4C1=CC=CC=C31)CCC2

InChiKey: RXPRRQLKFXBCSJ-GIVPXCGWSA-N

InChi: InChI=1S/C21H26N2O3/c1-3-20-10-6-11-22-12-9-15-14-7-4-5-8-16(14)23(17(15)18(20)22)21(25,13-20)19(24)26-2/h4-5,7-8,18,25H,3,6,9-13H2,1-2H3/t18-,20+,21+/m1/s1

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 25 mg/mL (70.53 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:

Vincamine (20, 40 and 80 μM; 24 hours) exerts a significant, concentration-dependent protective effect in LPS-treated human corneal epithelial cells (HCECs) cells. Vincamine (20, 40 and 80 μM; 24 hours) significantly reduces ROS level in a dose-dependent manner in LPS-treated human corneal epithelial cells (HCECs)cells. Additionally, after Vincamine administration, the levels of MDA is also significantly reduced while the levels of T-AOC, and SOD are increased in a dose-dependent manner. Vincamine (20, 40 and 80 μM; 24 hours) rescues TrxR activity in a dose-dependent manner in HCECs. However, the intracellular activities of Trx, GR and GPx are neither inhibited nor activated by both LPS and Vincaminer. Vincamine could activate GPR40 (EC50=6.28 µM) with DHA (GPR40 ligand) as a positive control (EC50=3.85 µM) in hGPR40-CHO cells.

In Vivo:

Vincamine (intraperitoneal injection; 15 and 30 mg/kg/day; 6 weeks) improves glucose tolerance in type 2 diabetic model mice. It effectively lowers the levels of fasting blood glucose and glycated hemoglobin. At the same time, it ameliorates oral glucose tolerance and elevated glucose-induced plasma insulin concentration without influence on basal insulin secretion in vivo.<.br>

References:

1. Te Du, et al. Vincamine as a GPR40 agonist improves glucose homeostasis in type 2 diabetic mice. J Endocrinol. 2019 Feb 1;240(2):195-214.
2. Li Wu, et al. Vincamine prevents lipopolysaccharide induced inflammation and oxidative stress via thioredoxin reductase activation in human corneal epithelial cells. Am J Transl Res. 2018 Jul 15;10(7):2195-2204. eCollection

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