Halobetasol propionate 是一种在皮肤外使用的合成类固醇,具有抗炎,止痒和收缩血管的活性。
产品描述
Halobetasol Propionate is the propionate salt form of halobetasol, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability.
体外活性
Halobetasol propionate is thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. The initial interaction, however, is due to the drug binding to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes.[1]
Cas No.
66852-54-8
分子式
C25H31ClF2O5
分子量
484.96
别名
卤贝他索丙酸酯;Ulobetasol propionate;BMY-30056;Halobetasol Propionate;CGP-14458;卤倍他索丙酸酯
储存和溶解度
Ethanol:36 mg/mL (74.2 mM)
H2O:<1 mgml
DMSO:90 mg/mL (185.6 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years