貨號	規(guī)格	價格	上海	北京	武漢	南京
S81251-5mg	98.2%	￥400.00 S81251-5mg ￥400.00 現(xiàn)貨	5 5	-	-	-
S81251-10mg	98.2%	￥680.00 S81251-10mg ￥680.00 現(xiàn)貨	6 6	-	-	-
S81251-25mg	98.2%	￥1440.00 S81251-25mg ￥1440.00 現(xiàn)貨	7 7	-	-	-

產(chǎn)品介紹

Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.

產(chǎn)品描述：

Vesatolimod (GS-9620) is a potent, selective and orally active agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.

靶點：

EC50: 291 nM (TLR7), 9 μM (TLR8);Apoptosis;?HCVProtease;?HBV;?TLR;?HIVProtease

體內(nèi)研究：

Single oral doses of Vesatolimod (GS-9620) at 0.3 and 1 mg/kg in uninfected chimpanzees demonstrates a dose- and exposure-related induction of serum IFN-α, select cytokines/chemokines, and IFN-stimulated genes (ISG) in the peripheral blood and liver. Following oral administration at 0.3 (n=3), and 1 mg/kg (n=3 and n=4), Vesatolimod (GS-9620) Cmax?is 3.6±3.5, 36.8±34.5, and 55.4±81.0 nM, respectively. Peak serum IFN responses occur at 8 h post-dose. The mean peak levels of induced serum IFN-α are 66 and 479 pg/mL at doses of 0.3 and 1 mg/kg, respectively. Vesatolimod (GS-9620) treatment induces ISG transcripts including ISG15, OAS-1, MX1, IP-10 (CXCL10), and I-TAC (CXCL11) in peripheral blood mononuclear cells (PBMC) at 0.3 mg/kg and in both PBMC and the liver at 1 mg/kg

參考文獻：

1. Rebbapragada I, et al. Molecular Determinants of GS-9620-Dependent TLR7 Activation. PLoS One. 2016 Jan 19;11(1):e0146835. 2. Lanford RE, et al. GS-9620, an Oral Agonist of Toll-Like Receptor-7, Induces Prolonged Suppression of Hepatitis B Virus in Chronically Infected Chimpanzees. Gastroenterology. 2013 Feb 13. pii: S0016-5085(13)00169-8. 3. D Tumas, et al. Preclinical Characterization of GS-9620, A Potent and Selective Oral TLR7 Agonist.

溶解性：

DMSO : ≥ 16.67 mg/mL (40.61 mM)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.436 ml	12.18 ml	24.36 ml
5 mM	0.487 ml	2.436 ml	4.872 ml
10 mM	0.244 ml	1.218 ml	2.436 ml
50 mM	0.049 ml	0.244 ml	0.487 ml

注意：

部分產(chǎn)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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