货号	规格	价格	上海	北京	珠海	重庆	武汉
S87931-5mg促销	98.40%	￥240.00 ￥192.00 S87931-5mg ￥192.00 现货	5 5	-	-	-	-
S87931-10mg促销	98.40%	￥390.00 ￥312.00 S87931-10mg ￥312.00 现货	6 6	-	-	-	-
S87931-25mg促销	98.40%	￥820.00 ￥656.00 S87931-25mg ￥656.00 现货	6 6	-	-	-	-
S87931-100mg促销	≥98%	￥2350.00 ￥1880.00 S87931-100mg ￥1880.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

SAR-20347 is an inhibitor of TYK2, JAK1/2/3 (IC50: 0.6/23/26/41 nM).

靶点：

JAK; Tyrosine Kinases;TyrosineKinases; JAK

体外研究：

SAR-20347 effectively inhibits IL-12-mediated STAT4 phosphorylation (TYK2-dependent, IC50: 126 nM) when NK-92 cells are stimulated with IL-12. In the culture media, cells without IL-12 have no measurable IFN-γ, while cells incubated with IL-12 and SAR-20347 demonstrate dose-dependent inhibition of IFN-γ production. SAR-20347 (maximum effect: 5 μM) dose-dependently inhibits the production of secreted embryonic alkaline phosphatase (SEAP).

体内研究：

Compared to vehicle-treated animals, SAR-20347 (60 mg/kg) inhibits the production of IFN-γ in the serum by 91%, demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. SAR-20347 markedly reduces IL-17 production as measured by average signal intensity, consistent with the gene expression analysis.

细胞实验：

Cells are plated in a 96-well v-bottom plate in starvation medium, incubated with SAR-20347 (0.5% DMSO) for 20 minutes at 37°C, 5% CO2, and stimulated with individual cytokines. P-STAT levels are measured in duplicate using MSD plates following the manufacturer's instructions (MSD).

动物实验：

Female 7 to 9-week old C57BL/6 mice are used. Mice are administered vehicle or 50 mg/kg SAR-20347 by oral gavage 30 minutes prior to application of 62.5 mg 5% imiquimod cream or control cream. Another dose of vehicle or 50 mg/kg SAR-20347 is given 5.5 hours following the first dose. This treatment is repeated for 5 days and on day 3 and 4, animals are injected with 100 uL saline to prevent dehydration. On the 6th day, the animals are euthanized and photographs are taken.

参考文献：

1. Works MG, et al. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87. 2. Kang X, Yang M, Shi Y, et al. Interleukin-15 facilitates muscle regeneration through modulation of fibro/adipogenic progenitors[J]. Cell Communication and Signaling. 2018 Jul 20;16(1):42.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.248 ml	11.24 ml	22.48 ml
5 mM	0.45 ml	2.248 ml	4.496 ml
10 mM	0.225 ml	1.124 ml	2.248 ml
50 mM	0.045 ml	0.225 ml	0.45 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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