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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
SHR0302
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1445987-21-2
- 规格：
10 mM * 1 mL/1 mg/5 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥4559.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥2000.0 |
| 规格： | 5 mg | 产品价格： | ￥5000.0 |
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Ivarmacitinib
CAS No. : 1445987-21-2
MCE 国际站：Ivarmacitinib
产品活性：Ivarmacitinib (SHR0302) 是一种有效的具有口服活性的 JAK 抑制剂，尤其是 JAK1 的抑制剂。Ivarmacitinib 对 JAK1 的选择性是 JAK2 的 10 倍以上，是 JAK3 的 77 倍，是 Tyk2 的 420 倍。Ivarmacitinib 抑制 JAK1-STAT3 磷酸化并诱导肝星状细胞凋亡 (apoptosis)。Ivarmacitinib 具有抗增殖和抗炎作用。
研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt | Apoptosis
In Vitro: 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.
In Vivo: 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.
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