产品
编 号：F165823
分子式：C18H22N8O2S
分子量：414.48
分子式：C18H22N8O2S
分子量：414.48
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1445987-21-2
产品详情
生物活性：
Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.
体内研究：
Ivarmacitinib (SHR0302; 0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats. Ivarmacitinib can inhibit the proliferation of T, B and fibroblast-like synoviocytes (FLS), and down-regulates cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppresses the proportion of Th17 and total B, and inhibits JAK1-STAT3 phosphorylation.Animal Model:Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)
Dosage:0.3 mg/kg,1.0 mg/kg, 3.0 mg/kg
Administration:Intragastric administration; twice a day; for 14 days
Result:Suppressed the severity of adjuvant-induced arthritis (AA) rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats.
体外研究：
Ivarmacitinib (SHR0302; 1 nM-10 μM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner.Ivarmacitinib (1 nM-10 μM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs.Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment induces the apoptosis of HSCs.Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 and Bax in HSCs, and decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway.
Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.
体内研究：
Ivarmacitinib (SHR0302; 0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats. Ivarmacitinib can inhibit the proliferation of T, B and fibroblast-like synoviocytes (FLS), and down-regulates cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppresses the proportion of Th17 and total B, and inhibits JAK1-STAT3 phosphorylation.Animal Model:Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)
Dosage:0.3 mg/kg,1.0 mg/kg, 3.0 mg/kg
Administration:Intragastric administration; twice a day; for 14 days
Result:Suppressed the severity of adjuvant-induced arthritis (AA) rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats.
体外研究：
Ivarmacitinib (SHR0302; 1 nM-10 μM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner.Ivarmacitinib (1 nM-10 μM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs.Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment induces the apoptosis of HSCs.Ivarmacitinib (1 nM-10 μM; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 and Bax in HSCs, and decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备