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Imidazole antimycotic and cytochrome P450 inhibitor. Inhibits Ca2+-activated K+ current (IC50 = 3 μM) and L-type Ca2+ current; increases the firing rate of action potentials. Exhibits antiproliferative activity in vitro and in vivo. Also an inverse agonist of the human constitutive androstane receptor (hCAR).
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 344.84. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.9 mL||14.5 mL||29 mL|
|5 mM||0.58 mL||2.9 mL||5.8 mL|
|10 mM||0.29 mL||1.45 mL||2.9 mL|
|50 mM||0.06 mL||0.29 mL||0.58 mL|
References are publications that support the biological activity of the product.
Snajdrova et al (1998) Clomitrazole, an antimycotic drug, inhibits the sarcoplasmic reticulum calcium pump and contractile function in heart muscle. J.Biol.Chem. 273 28032 PMID: 9774419
Wu et al (1999) Inhibition of Ca2+-activated K+ current by clotrimazole in rat anterior pituitary GH3 cells. Neuropharmacology 38 979 PMID: 10428416
Thomas et al (1999) The antifungal antibiotic clotrimazole potently inhibits L-type calcium current in guinea-pig ventricular myocytes. Br.J.Pharmacol. 126 1531 PMID: 10323582
Lempiainen et al (2005) Antagonist- and inverse agonist-driven interactions of the vitamin D receptor and the constitutive androstane receptor with corepressor protein. Mol.Endocrinol. 19 2258 PMID: 15905360
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