A general calcium channel blocker
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Mibefradil (hydrochloride)

Item No. 15037

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(1S,2S)-2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl ester 2-methoxy-acetic acid, dihydrochloride
CAS Number
116666-63-8
Synonyms
  • Posicor
  • Ro 40-5967
Molecular Formula
C29H38FN3O3 • 2HCl
Formula Weight
568.6
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 16 mg/mlDMSO: 14 mg/mlEthanol: 16 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
242, 270, 276 nm
SMILES
CN(CCCC1=NC2=C(C=CC=C2)N1)CC[C@]([C@H]3C(C)C)(CCC4=CC(F)=CC=C34)OC(COC)=O.Cl.Cl
InChi Code
InChI=1S/C29H38FN3O3.2ClH/c1-20(2)28-23-12-11-22(30)18-21(23)13-14-29(28,36-27(34)19-35-4)15-17-33(3)16-7-10-26-31-24-8-5-6-9-25(24)32-26;;/h5-6,8-9,11-12,18,20,28H,7,10,13-17,19H2,1-4H3,(H,31,32);2*1H/t28-,29-;;/m0../s1
InChi Key
MTJLQTFHJIHXIX-GDUXWEAWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $117

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    10 mg

    $206

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    25 mg

    $484

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    50 mg

    $909

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    Product Description

    Mibefradil is a general calcium channel blocker that shows modest selectivity for T-type channels over L-type channels (IC50 = 2.7 and 18.6 μM, respectively).1,2,3 It is a potent vasodilator, increasing coronary artery flow with an EC50 value of 54 nM.2 Mibefradil has minimal negative inotropic effects, supporting its use as an anti-hypertensive agent.2,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bezprozvanny, I., and Tsien, R.W. Voltage-dependent blockade of diverse types of voltage-gated Ca2+ channels expressed in Xenopus oocytes by the Ca2+ channel antagonist mibefradil (Ro 40-5967). Mol. Pharmacol. 48(3), 540-549 (1995).

    2. Osterrieder, W., and Holck, M. In vitro pharmacologic profile of Ro 40-5967, a novel Ca2+ channel blocker with potent vasodilator but weak inotropic action. J. Biomed. Sci. 13(5), 754-759 (1989).

    3. Mehrke, G., Zong, X.G., Flockerzi, V., et al. The Ca++-channel blocker Ro 40-5967 blocks differently T-type and L-type Ca++ channels. J. Pharmacol. Exp. Ther. 271(3), 1483-1488 (1994).

    4. Véniant, M., Clozel, J.P., Hess, P., et al. Hemodynamic profile of Ro 40-5967 in conscious rats: Comparison with diltiazem, verapamil, and amlodipine. J. Biomed. Sci. 18(10), S55-S58 (1991).