货号	规格	价格	上海	北京	珠海	重庆	武汉
S82245-1mg买3赠1	99.90%	￥200.00 S82245-1mg ￥200.00 现货（买3赠1）	8 8	-	-	-	-
S82245-5mg买3赠1	99.90%	￥275.00 S82245-5mg ￥275.00 现货（买3赠1）	9 9	-	-	-	-
S82245-10mg买3赠1	99.90%	￥390.00 S82245-10mg ￥390.00 现货（买3赠1）	8 8	-	-	-	-
S82245-25mg买3赠1	99.90%	￥590.00 S82245-25mg ￥590.00 现货（买3赠1）	8 8	-	-	-	-
S82245-50mg买3赠1	99.90%	￥970.00 S82245-50mg ￥970.00 现货（买3赠1）	8 8	-	-	-	-
S82245-100mg买3赠1	99.90%	￥1470.00 S82245-100mg ￥1470.00 现货（买3赠1）	7 7	-	-	-	-
S82245-1g买3赠1	99.90%	￥4980.00 S82245-1g ￥4980.00 现货（买3赠1）	3 3	-	-	-	-

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产品描述：

Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.

靶点：

JAK2:5.7 nM (IC50);JAK1:5.9 nM (IC50);Tyk2:53 nM (IC50);JAK3:560 nM (IC50);TyrosineKinases; JAK

体外研究：

In cell-based assays, Baricitinib phosphate (INCB028050 phosphate) proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC50=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC50 value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM

体内研究：

Baricitinib phosphate (INCB028050 phosphate) treatment, compares with vehicle, inhibits the increase in hind paw volumes during the 2 wk of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 or 10 mg/kg. Because baseline paw volume measurements are taken on treatment day 0-in animals with significant signs of disease-it is possible to have >100% inhibition in animals showing marked improvement in swelling. Baricitinib (0.7 mg/day) treated mice exhibits substantially reduced inflammation as assessed by H&E staining, reduced CD8 infiltration, and reduced MHC class I and class II expression when compared with vehicle-control treated mice. CD8+NKG2D+ cells, critical effectors of disease in murine and human alopecia areata (AA), are greatly diminished in Baricitinib treated mice compare with vehicle control treated mice

参考文献：

1. Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307. 2. Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.13 ml	10.652 ml	21.303 ml
5 mM	0.426 ml	2.13 ml	4.261 ml
10 mM	0.213 ml	1.065 ml	2.13 ml
50 mM	0.043 ml	0.213 ml	0.426 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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Baricitinib (phosphate)