| Identification | Back Directory | [Name]
2-Propenamide, N-[3-[[2-[[3-chloro-4-[3-(4-morpholinyl)propoxy]phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]- | [CAS]
2307699-34-7 | [Synonyms]
Thi-DPPY
2-Propenamide, N-[3-[[2-[[3-chloro-4-[3-(4-morpholinyl)propoxy]phenyl]amino]thieno[3,2-d]pyrimidin-4-yl]oxy]phenyl]- | [Molecular Formula]
C28H28ClN5O4S | [MOL File]
2307699-34-7.mol | [Molecular Weight]
566.07 |
| Hazard Information | Back Directory | [Uses]
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF)[1]. | [in vivo]
DPPY (30, 60 mg/kg; i.g., once daily for 14 days) shows anti-IPF agents on the lung morphology and lung coefficient in mouse model[1].
DPPY (30, 60 mg/kg) significantly decreases the expression of IL-6, IL-17A, TNF-α and MDA in lung tissue in a dose dependent manner[1]. | Animal Model: | 5-6 week old, 20-25 g, C57BL mice (BLM-induced pulmonary inflammation and pulmonary fibrosis model)[1] | | Dosage: | 30, 60 mg/kg | | Administration: | I.g.; once daily for 14 days | | Result: | Attenuated the pulmonary morphology changes and reduced the collagen disposition induced by BLM in mouse lung. |
| [IC 50]
JAK3: 1.38 nM (IC50); BTK: 62.4 nM (IC50) | [References]
[1] Zhu Y, et al. Synthesis and biological activity of thieno[3,2-d]pyrimidines as potent JAK3 inhibitors for the treatment of idiopathic pulmonary fibrosis. Bioorg Med Chem. 2020 Jan 15;28(2):115254. DOI:10.1016/j.bmc.2019.115254 |
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