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GS-9620 Sale

(Synonyms: 维沙莫德; GS-9620) 目录号 : GC12555

A TLR7 agonist

GS-9620 Chemical Structure

Cas No.:1228585-88-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥534.00
现货
5mg
¥495.00
现货
10mg
¥945.00
现货
50mg
¥2,673.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1]:

Cell lines

Peripheral blood mononuclear cells (PBMCs) or plasmacytoid dendritic cells (pDCs)

Preparation method

Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

14 ~ 66 nM

Applications

In human and cynomolgus monkey PBMCs and/or pDCs, GS-9620 induced interferon (IFN)-alpha and other cytokines, with a minimum effective concentration ranging from 14 to 66 nM in humans and with 5-fold less potency in monkeys.

Animal experiment [1]:

Animal models

Cynomolgus monkeys

Dosage form

single doses of 0.1 ~ 2.0 mg, daily doses of 0.1 ~ 1.0 mg for 7 days or every other day doses of 0.05 ~ 1.5 mg for 28 days; p.o.

Applications

In cynomolgus monkeys, GS-9620 was well tolerated even at the highest oral doses (1.5 mg every other day for 28 days). GS-9620 increased IFN-alpha, immunomodulatory cytokines, chemokines and peripheral blood cell IFN stimulated genes (ISGs) in a dose-dependent manner. In addition, there was no evidence of tachyphylaxis following every other day dosing, and oral administration resulted in limited systemic bioavailability but high oral absorption.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Turnas P, Zheng X, Lu B, et al. 1129 Preclinical characterization of GS-9620, a potent and selective oral TLR7 agonist[J]. Journal of Hepatology, 2011, 54: S446-S447.

产品描述

GS-9620 is an orally active TLR7 agonist with EC50 of 291 nM. [1]
Toll-like receptor 7 (TLR7) is a pathogen recognition receptor which plays an important role in the detection of, and the innate immune response to, pathogens. TLR7 signaling is predominantly activated by viral single-stranded RNA and is localized within the endolysosomal compartments of plasmacytoid dendritic cells (pDCs) and B lymphocytes in humans and non-human primates. Activation of pDCs plays an important role in the progress of innate response to viral pathogens and are involved in the majority of type I interferon (IFN) production during the acute phase of an infection by viruses. The induction and secretion of endogenous IFNs, including IFN-α and IFN- β, also induce the development of an efficient adaptive immunological response. Interferons induce the transcription of interferon-stimulated genes (ISGs) which generate an antiviral state within cells, as well as induce the production of other cytokines and chemokines which facilitate intercellular communication and cellular trafficking. GS-9620 could activate TLR7 signaling in immune cells to induce clearance of virus infected cells. [1, 2]
GS-9620 selectively induces IFN-α, cytokines and chemokines. The minimum effective concentrations for IFN-α induction were similar in pDCs and in PBMCs from HCV-positive donors. GS-9620 demonstrates an EC50 of 291 nM for human TLR7, which is 30-fold selectivity over TLR8 with EC50 of 9 μM. [1]
GS-9620 was administered to HBV infected chimpanzees for 8 weeks with an interval of 1 week. Consequently, serum concentrations of HBV surface antigen and HBV antigen, and the number of HBV antigen–positive hepatocytes, were decreased as hepatocyte apoptosis increased. In a phase 1 clinical trial to evaluate the safety and tolerability of GS-9620, treatment of GS-9620 results in dose dependent increases in select cytokines, chemokines, and ISGs beginning at 2mg and is safe in a single dose up to 12mg. Increases in percentages of immunocytes, like T cells, B cells and NK cells, expressing CD69 were also noted in subjects receiving GS-9620 treatment. [2, 3]
References:
[1]. Turnas P, Zheng X, Lu B, et al. 1129 Preclinical characterization of GS-9620, a potent and selective oral TLR7 agonist[J]. Journal of Hepatology, 2011, 54: S446-S447.
[2]. Lanford R E, Guerra B, Chavez D, et al. GS-9620, an oral agonist of Toll-like receptor-7, induces prolonged suppression of hepatitis B virus in chronically infected chimpanzees[J]. Gastroenterology, 2013, 144(7): 1508-1517. e10.
[3]. Lopatin U, Wolfgang G, Kimberlin R, et al. 737 A phase-i, randomized, double-blind, placebo-controlled study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of single escalating oral doses of GS-9620 in healthy subjects[J]. Journal of Hepatology, 2011, 54: S296.

Chemical Properties

Cas No. 1228585-88-3 SDF
别名 维沙莫德; GS-9620
化学名 4-amino-2-butoxy-8-[[3-(pyrrolidin-1-ylmethyl)phenyl]methyl]-5,7-dihydropteridin-6-one
Canonical SMILES CCCCOC1=NC2=C(C(=N1)N)NC(=O)CN2CC3=CC(=CC=C3)CN4CCCC4
分子式 C22H30N6O2 分子量 410.51
溶解度 ≥ 20.55 mg/mL in DMSO, ≥ 9.9 mg/mL in EtOH with ultrasonic and warming 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.436 mL 12.18 mL 24.3599 mL
5 mM 0.4872 mL 2.436 mL 4.872 mL
10 mM 0.2436 mL 1.218 mL 2.436 mL
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