貨號	規格	價格	上海	北京	武漢	南京
S80165-2mg	99.7%	￥50.00 S80165-2mg ￥50.00 現貨	10 10	-	-	-
S80165-5mg	99.7%	￥75.00 S80165-5mg ￥75.00 現貨	9 9	-	-	-
S80165-10mg	99.7%	￥125.00 S80165-10mg ￥125.00 現貨	7 7	-	-	-
S80165-25mg	99.7%	￥260.00 S80165-25mg ￥260.00 現貨	5 5	-	-	-
S80165-50mg	99.7%	￥420.00 S80165-50mg ￥420.00 現貨	5 5	-	-	-
S80165-100mg	99.7%	￥600.00 S80165-100mg ￥600.00 現貨	4 4	-	-	-

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產品介紹

Filgotinib (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively

產品描述：

Filgotinib (GLPG0634) is a selective and orally active JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively

靶點：

JAK1:10 nM (IC50);JAK2:28 nM (IC50);Tyk2:116 nM (IC50);JAK3:810 nM (IC50);TyrosineKinases;JAK

體外研究：

Filgotinib (GLPG0634) dose-dependently inhibits the differentiation of Th2 cells mediated by IL-4, a cytokine that signals through JAK1 and JAK3. Filgotinib also inhibits Th1 differentiation with similar potencies of 1 μM or lower. Filgotinib (GLPG0634) does not inhibit JAK2 homodimer-mediated signaling induced by EPO or PRL (IC50 > 10 μM)

體內研究：

Filgotinib (GLPG0634; 3, 10, 30 mg/kg, p.o.) dose-dependently prevents disease progression in the therapeutic rat CIA model. Filgotinib (50 mg/kg, o.p.) protects bone and cartilage from degradation, effectively reduces infiltration of T cells (CD3+ cells) and macrophages (F4/80+ cells) in the paw, and decreases the serum levels of all cytokines and chemokines measured, including IL-6, IP-10, XCL1, and MCP-1. Filgotinib (GLPG0634; 0.1 and 0.3 mg/kg) shows efficacy in the rat CIA model

參考文獻：

1. Van Rompaey L, et al. Preclinical characterization of GLPG0634, a selective inhibitor of JAK1, for the treatment of inflammatory diseases. J Immunol. 2013, 191(7), 3568-3577. 2. Menet CJ, et al. Triazolopyridines as Selective JAK1 Inhibitors: From Hit Identification to GLPG0634. J Med Chem. 2014 Nov 17.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.35 ml	11.751 ml	23.502 ml
5 mM	0.47 ml	2.35 ml	4.7 ml
10 mM	0.235 ml	1.175 ml	2.35 ml
50 mM	0.047 ml	0.235 ml	0.47 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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