(R) -Verapamil

(R) -Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil. (R) -Verapamil has a relatively low affinity for L-type calcium channels (Cav1.2) (IC50 > 300 μM), and its IC50 for sodium channels (sodium channel) is 3.19 μM. (R) -Verapamil exhibits SSTR2 agonistic activity, with an EC50 of 1.3 μM. (R) -Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R) -Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp)[2][3].

38321-02-7

Dexverapamil

12352005

H302-H315-H319-H335

Apoptosis; Arrestin; Calcium Channel; P-glycoprotein; Potassium Channel; Somatostatin Receptor

Apoptosis; GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Metabolism-protein/nucleotide metabolism

Inflammation/Immunology; Metabolic Disease

COC(C=C1CCN(C)CCC[C@](C#N)(C2=CC(OC)=C(C=C2)OC)C(C)C)=C(C=C1)OC

C27H38N2O4

454.60

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

[1]Chen YS, et al. Evaluating the antidiabetic effects of R-verapamil in type 1 and type 2 diabetes mellitus mouse models. PLoS One. 2021 Aug 6;16 (8) :e0255405.|[2]Busse D, et al. Cardiovascular effects of (R) - and (S) -verapamil and racemic verapamil in humans: a placebo-controlled study. Eur J Clin Pharmacol. 2006 Aug;62 (8) :613-9. |[3]Luurtsema G, et al. (R) - and (S) -[11C]verapamil as PET-tracers for measuring P-glycoprotein function: in vitro and in vivo evaluation. Nucl Med Biol. 2003 Oct;30 (7) :747-51.

Room temperature

http://file.medchemexpress.com/batch_PDF/HY-Z15823/

Reference compound1

No Development Reported