(R)-Verapamil  (Synonyms: Dexverapamil)

(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Ca_v1.2) (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)^[1][2][3].

454.60

C₂₇H₃₈N₂O₄

38321-02-7

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]