| 体内研究: |
S18-000003 (30-100 mg/kg; p.o.) inhibits IL-17 production in the skin of IL-23-treated mice in a dose-dependent manner. S18-000003 (0.1-8%; 100mL; topically administration once daily for 14 days) ameliorates psoriasis-like lesions in TPA-induced K14.Stat3C transgenic mice, and has little impact on the thymus. S18-000003 (0.5 mg/kg; i.v.) exhibits the half-life (3.2 h), AUC (1930 ng h/mL), CLtot (4.33 mL/min/kg) and Vdss in rats. S18-000003 (1 mg/kg; p.o.) exhibits the oral bioavailability (54.5%), Cmax (185 ng/mL), AUC (2110 ng h/mL) and Tmax (4 h) in rats. |
| 参考文献: |
1. Sasaki Y, et, al. Discovery of a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor, S18-000003. Bioorg Med Chem Lett. 2018 Dec 1;28(22):3549-3553. 2. Imura C, et, al. A novel RORγt inhibitor is a potential therapeutic agent for the topical treatment of psoriasis with low risk of thymic aberrations. J Dermatol Sci. 2019 Mar;93(3):176-185. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.928 ml |
9.642 ml |
19.285 ml |
| 5 mM |
0.386 ml |
1.928 ml |
3.857 ml |
| 10 mM |
0.193 ml |
0.964 ml |
1.928 ml |
| 50 mM |
0.039 ml |
0.193 ml |
0.386 ml |
|
| 注意: |
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