Thi-DPPY (compound 8e) 是一种有效且具有口服活性的JAK3抑制剂,对 BTK、JAK 的IC50值分别为62.4, 1.38 nM。Thi-DPPY 对 HBE 细胞具有抗增殖活性。Thi-DPPY 在体内显示出抗炎活性。Thi-DPPY 具有研究特发性肺纤维化(IPF)的潜力。
产品描述
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC 50 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].
体外活性
DPPY (compound 8e) shows anti-proliferative activity against HBE (human bronchial epithelia) cells with an IC 50 of 39.0 μM [1].
体内活性
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.
Cas No.
2307699-34-7
分子式
C28H28ClN5O4S
分子量
566.07
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years