Bioactivity | Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages[1][2][3]. |
Invitro | Metabolism of Beclomethasone dipropionate to 17-BMP is an important activation step. Beclomethasone 17-propionate inhibits LPS-stimulated CXCL8, TNFα and IL-6. The EC50 values of Beclomethasone 17-propionate for IL-6, TNFα and CXCL8 were 0.05 nM, 0.01 nM and 0.1 nM, respectively. Beclomethasone 17-propionate evokes upregulation of the GR dependent genes FKBP51 and GILZ[3]. |
Name | Beclomethasone 17-propionate |
CAS | 5534-18-9 |
Formula | C25H33ClO6 |
Molar Mass | 464.98 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
Reference | [1]. Würthwein G, et al. Activation of beclomethasone dipropionate by hydrolysis to beclomethasone-17-monopropionate. Biopharm Drug Dispos. 1990 Jul;11(5):381-94. [2]. Roberts JK, et al. Metabolism of beclomethasone dipropionate by cytochrome P450 3A enzymes. J Pharmacol Exp Ther. 2013 May;345(2):308-16. [3]. Plumb J, et al. Evaluation of glucocorticoid receptor function in COPD lung macrophages using beclomethasone-17-monopropionate. PLoS One. 2013 May 21;8(5):e64257. |