BI 1015550 dihydrate_product_DataBase

Bioactivity	BI 1015550 (dihydrate) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. BI 1015550 (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD)[1][2].
Invitro	BI 1015550 (dihydrate) 在人 PBMCs 中抑制脂多糖 (Lipopolysaccharides，HY-D1056) 诱导的 TNF-α 的释放，植物血凝素 P (Phytohemagglutinin P，HY-N7038A) 诱导的 IL-2 的释放，IC50 值分别为 35 nM 和 9 nM[2]。BI 1015550 (dihydrate) 在大鼠全血中抑制 TNF-α 的释放，IC50 值为 91 nM[2]。
In Vivo	BI 1015550 (dihydrate) (Example 2) (0、0.3、1.0 和 3.0 mg/kg；口服；单剂量) 在 1.0 mg/kg 时弱化了大鼠的肠道转运，但不显著影响体重[1]。BI 1015550 (dihydrate) 能预防大鼠肺组织的炎症，ED50 值为 0.1 mg/kg[1]。BI 1015550 (dihydrate) (0.01、0.1 和 1.0 mg/kg；口服；单剂量) 在小鼠血浆中以剂量依赖性方式减少了脂多糖 (Lipopolysaccharides，HY-D1056) 诱导的 TNF-α 的释放[2]。BI 1015550 (dihydrate) (0.1、0.3 和 1.0 mg/kg；口服；单剂量) 抑制脂多糖诱导的中性粒细胞进入雄性 Suncus Murinus 和 Wistar 大鼠支气管肺泡灌洗液[2]。BI 1015550 (dihydrate) (2.5 mg/kg 和 12.5 mg/kg；口服；一天 2 次持续 6 天) 有效改善了博来霉素 (Bleomycin，HY-108345) 对小鼠的损害[2]。 Animal Model:
Name	BI 1015550 dihydrate
Formula	C20H29ClN6O4S
Molar Mass	485.00
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Pouzet P A, et al. Piperidino-dihydrothienopyrimidine sulfoxides and their use for treating COPD and asthma. United States. US9150586. [2]. Herrmann FE, et al. BI 1015550 is a PDE4B Inhibitor and a Clinical Drug Candidate for the Oral Treatment of Idiopathic Pulmonary Fibrosis. Front Pharmacol. 2022 Apr 20;13:838449.

PeptideDB

BI 1015550 dihydrate

CAS: F: C20H29ClN6O4S W: 485.00