货号	规格	价格	上海	北京	珠海	重庆	武汉
S88727-2mg买3赠1	99.90%	￥80.00 S88727-2mg ￥80.00 现货（买3赠1）	5 5	-	-	-	-
S88727-5mg	99.90%	￥110.00 S88727-5mg ￥110.00 现货	5 5	-	-	-	-
S88727-10mg	99.90%	￥160.00 S88727-10mg ￥160.00 现货	4 4	-	-	-	-
S88727-25mg	99.90%	￥260.00 S88727-25mg ￥260.00 现货	6 6	-	-	-	-
S88727-50mg	≥98%	￥470.00 S88727-50mg ￥470.00 2-3天	0 货期：2-3天	-	-	-	-
S88727-100mg	≥98%	￥640.00 S88727-100mg ￥640.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively. Apilimod is a potent and highly selective PIKfyve inhibitor.

靶点：

IL-4;IL-5;IL-8;IL-12;IL-23;ILReceptor; PI3K; Interleukin

体外研究：

Apilimod inhibits IFN-γ production induced by either IFN-γ/SAC or SAC in human PBMCs, with an IC50 of approximately 20 nM. Apilimod show some inhibition against IFN-γ/SAC-induced TNF-α and ConA-induced IL-5 from human PBMCs at high concentrations, but no suppressive effect against IL-1β, IL-2, IL-4, IL-8, and IL-18 in all cultures tested. The p35 and p40 promoter-driven luciferase activities are significantly induced after stimulation with IFN-γ/LPS or IFN-γ/SAC, and are completely suppressed by 100 nM Apilimod

体内研究：

Apilimod (10 mg/kg, p.o.) is effective not only when administered throughout the entire experiment, but also when administration is initiated on day 30 when disease is clearly measurable but not maximal. Apilimod causes a significant reduction in cell number only in the Th1 model, with an average percentage of inhibition of 51%±8% relative to the vehicle control. Apilimod treatment has no effect in the Th2 setting. Apilimod (5 or 20 mg/kg, p.o.) reduces the level of IL-12 p40 in serum without altering body weight in EAU mice. Oral administration of Apilimod reduces the severity of experimental autoimmune uveoretinitis (EAU) by clinical and histopathological analysis

参考文献：

1. Wada Y, et al. Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood. 2007 Feb 1;109(3):1156-64. 2. Billich A. Drug evaluation: apilimod, an oral IL-12/IL-23 inhibitor for the treatment of autoimmune diseases and common variable immunodeficiency.IDrugs. 2007 Jan;10(1):53-9. 3. Keino H, et al. Therapeutic effect of the potent IL-12/IL-23 inhibitor STA-5326 on experimental autoimmune uveoretinitis. Arthritis Res Ther. 2008;10(5):R122.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.637 ml	8.187 ml	16.375 ml
5 mM	0.327 ml	1.637 ml	3.275 ml
10 mM	0.164 ml	0.819 ml	1.637 ml
50 mM	0.033 ml	0.164 ml	0.327 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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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

APILIMOD MESYLATE

ApiliMod (Mesylate)；STA 5326 mesylate

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)