Bioactivity | Clobetasol propionate is a potent and selective CYP3A5 inhibitor with an IC50 of 0.206 μM. Clobetasol propionate has no inhibiting on CYP3A4 or other major CYPs. Clobetasol propionate is a corticosteroid and has the potential for psoriasis and other dermatoses research[1][2][3]. | ||||||||||||
Invitro | Clobetasol propionate has an IC50 of 15.6 μM for CYP3A4[1]. Clobetasol propionate (1 μM; 24 hours) selectively inhibits CYP3A5 and does not increase the protein level of CYP3A4. Clobetasol propionate does not affect cell growth in any cell line (AsPC-1 wild-type (WT), AsPC-1CYP3A5–/– cells with CYP3A5 overexpression (“3A5–/– + 3A5OE” cells), and AsPC-1CYP3A5–/– cells with CYP3A4 overexpression (“3A5–/– + 3A4OE” cells))[1]. | ||||||||||||
In Vivo | Clobetasol propionate (applied topically; daily for 14 days) reduces the epidermal thickness of both normal and psoriatic skin in human psoriatic skin-SCID mouse transplant model topical application[3]. | ||||||||||||
Name | Clobetasol propionate | ||||||||||||
CAS | 25122-46-7 | ||||||||||||
Formula | C25H32ClFO5 | ||||||||||||
Molar Mass | 466.97 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. William C Wright, et al. Clobetasol Propionate Is a Heme-Mediated Selective Inhibitor of Human Cytochrome P450 3A5. J Med Chem. 2020 Feb 13;63(3):1415-1433. [2]. Steven R Feldman, et al. Topical clobetasol propionate in the treatment of psoriasis: a review of newer formulations. Am J Clin Dermatol. 2009;10(6):397-406. [3]. M Zeigler, et al. Anti-CD11a ameliorates disease in the human psoriatic skin-SCID mouse transplant model: comparison of antibody to CD11a with Cyclosporin A and clobetasol propionate. Lab Invest. 2001 Sep;81(9):1253-61. |