克立硼罗 T4285

Product Introduction
Bioactivity


英文名: Crisaborole

描述: Crisaborole (AN-2728) 是一种有效的 PDE4和 cytokine 释放抑制剂，能够抑制 PDE4(IC50=0.49 μM)。

体外活性: AN-2728 inhibits PDE isozymes PDE1A3, PDE3Cat , PDE4Cat and PDE7A1 with IC50 values of 6.1, 6.4, 0.11 and 0.73 μM. AN-2728 inhibits PDE4, TNF-α, IL-2, IFN-γ, IL-5 and IL-10 with IC50 values of 0.49, 0.54, 0.61, 0.83, 2.4 and 5.3 μM. AN-2728 shows the most potent activity against PDE4 catalytic domain, but it also shows inhibition against PDE1A3, PDE3Cat, and PDE7A1. Crystallography reveals that interaction of benzoxaboroles with the hydrophobic pocket in the PDE4 catalytic domain increase their affinity for PDE4. These benzoxaboroles strongly suppresses the secretion of cytokines associated with Ps and AD.

体内活性: AN-2728 is reported to be well tolerated and to demonstrate significant effects on markers of efficacy, with results that were comparable to positive controls in clinical trials. AN-2728 shows significant inhibition against the ear edema caused by phorbol ester after dosing at 1 mg/ear×2 (78% and 68%, respectively). The efficacy is comparable to that of dexamethasone, suggesting that AN-2728 has good anti-inflammatory activity as well as skin penetration.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (199.16 mM)


关键字: Inhibitor | inhibit | AN 2728 | PF06930164 | AN2728 | Crisaborole | PF 06930164 | Phosphodiesterase (PDE)

相关产品: ICI 63197 | ML-030 | Zatolmilast | Verofylline | VP3.15 dihydrobromide | Ensifentrine | Carbazeran | PF-04957325 | T-0156 | Roflumilast

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Approved Drug Library | ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Clinical Compound Library | Inhibitor Library | Pediatric Drug Library | EMA Approved Drug Library | Anti-Cardiovascular Disease Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途