| Identification | Back Directory | [Name]
[1-({(5R)-2-[4-(5-chloropyrimidin-2-yl)piperidin-1-yl]-5-oxido-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl}amino)cyclobutyl]methanol | [CAS]
1423719-30-5 | [Synonyms]
BI 1015550
[1-({(5R)-2-[4-(5-chloropyrimidin-2-yl)piperidin-1-yl]-5-oxido-6,7-dihydrothieno[3,2-d]pyrimidin-4-yl}amino)cyclobutyl]methanol
(5R)-2-[4-(5-Chloropyrimidin-2-yl)piperidin-1-yl]-4-[[1-(hydroxymethyl)cyclobutyl]amino]-6,7-dihydro-5H-5lambda4-thieno[3,2-d]pyrimidin-5-one | [EINECS(EC#)]
823-454-9 | [Molecular Formula]
C20H26ClN6O2S- | [MOL File]
1423719-30-5.mol | [Molecular Weight]
449.977 |
| Hazard Information | Back Directory | [Uses]
Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD)[1][2]. | [in vivo]
Nerandomilast (Example 2) (0, 0.3, 1.0 and 3.0 mg/kg; p.o.; single dose) weakens intestinal transport in rats at 1.0 mg/kg without significantly affecting body weight[1].
Nerandomilast prevents inflammation in rat lung tissue with an ED50 value of 0.1 mg/kg[1].
Nerandomilast (0.01, 0.1 and 1.0 mg/kg; p.o.; single dose) reduces the Lipopolysaccharides (HY-D1056) induced TNF-α release with dose-dependent manner in mice plasma[2].
Nerandomilast (0.1, 0.3 and 1.0 mg/kg; p.o.; single dose) inhibits lipopolysaccharides induced neutrophil entry into bronchoalveolar lavage fluid of male Suncus Murinus and Wistar rats[2].
Nerandomilast (2.5 mg/kg and 12.5 mg/kg; p.o.; twice daily for 6 days) effectively improves the damage of Bleomycin (HY-108345) to mice[2].
| Animal Model: | Rats[1]. | | Dosage: | 0, 0.3, 1.0 and 3.0 mg/kg. | | Administration: | Oral gavage; single dose. | | Result: | Had minimal toxic and side effects on the intestines and stomach of rats, demonstrating biosafety. |
| Animal Model: | Male Suncus Murinus and Wistar rats; mice[2]. | | Dosage: | 0.01, 0.1, 0.3, 1.0, 2.5 or 12.5 mg/kg. | | Administration: | Oral gavage; single dose or twice daily for 6 days. | | Result: | Effectively improved inflammation in lung tissue and reduced the pro-inflammatory factor TNF-α release. |
| [References]
[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. DOI:10.3389/fphar.2022.838449 |
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