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首页 / 抑制剂/激动剂 / 免疫/炎症 / TLR / Vesatolimod/维沙莫德

Vesatolimod/维沙莫德 {[allProObj[0].p_purity_real_show]}

货号：A420074 同义名： GS-9620

GS-9620 is a selective agonist of Toll-like receptor 7 (TLR-7) in chimpanzees and has anti-HBV infection activity.

Vesatolimod/维沙莫德 化学结构 CAS号：1228585-88-3
Vesatolimod/维沙莫德 化学结构
CAS号：1228585-88-3
Vesatolimod/维沙莫德 3D分子结构
CAS号：1228585-88-3
Vesatolimod/维沙莫德 化学结构 CAS号：1228585-88-3
Vesatolimod/维沙莫德 3D分子结构 CAS号：1228585-88-3
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Vesatolimod/维沙莫德 纯度/质量文件 产品仅供科研

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Vesatolimod/维沙莫德 生物活性

描述 Toll like receptors are a membrane-based family which could modulate the immune responses by detecting distinct pathogen-associated molecular patterns on infectious agents[7]. GS-9620 is an orally bioavailable small-molecule TLR7 agonist with EC50 value of 130 nM and 4,000 nM for TLR7 and TLR8, respectively[8]. On the PBMCs from ART-suppressed HIV infected patients, the GS-9620 was added to the cells at 100 and 1000 nM and incubated for four days. The HIV RNA level in the cell culture supernatants was 1.7-1.9-fold increased after the treatment of GS-9620 compared with vehicle control. After two days of GS-9620 treatment on PBMCs, the IFN-α level as well as some proinflammatory cytokines and chemokines such as MCP-1, I-TAC, IL-1RA, IL-6, IL-10, MIP-1β, IP-10, and MIP-1α increased significantly as measured by multiplex immunoassays in the cell culture supernatant[9]. GS-9620 was administered to chimpanzees with chronic HBV infection every other day (3 times each week) for 4 weeks at 1 mg/kg and, after a 1 week rest, for 4 weeks at 2 mg/kg. The HBV DNA in serum and liver determined by qRCR declined gradually after the treatment. The administration of GS-9620 also induced production of IFN-α and other cytokines and chemokines, and activated ISGs, natural killer cells, and lymphocyte subsets measured by ELISA and flow cytometry[10].
作用机制 The GS-9620 can bind to the TLR7 in a pH responsive manner. The binding pocket of the GS-9620 may be formed by amino acids D555 and D557 in LRR17 region from one monomer and amino acids Y356 in LRR11 domain and F408 in LRR13 domain from the second monomer together[11].

Vesatolimod/维沙莫德 动物研究

Dose Chimpanzee: 0.3 mg/kg, 1 mg/kg[4] (p.o.) Woodchuck: 1 mg/kg -10 mg/kg[6] (p.o.)
Administration p.o.

Vesatolimod/维沙莫德 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01590654 Hepatitis B Phase 1 Completed - -
NCT03060447 HIV-1 Infection Phase 1 Active, not recruiting July 2020 United States, California ... 展开 >> Mills Clinical Research Los Angeles, California, United States, 90069 Zuckerberg San Francisco General San Francisco, California, United States, 94110 United States, Florida Midway Immunology & Research Center Fort Pierce, Florida, United States, 34982 Orlando Immunology Center Orlando, Florida, United States, 32803 United States, Texas Central Texas Clinical Research Austin, Texas, United States, 78705 United States, Washington Peter Shalit, MD Seattle, Washington, United States, 98104 收起 <<
NCT02258581 - Terminated - -

Vesatolimod/维沙莫德 参考文献

[1]The GS-9620 can bind to the TLR7 in a pH responsive manner. The binding pocket of the GS-9620 may be formed by amino acids D555 and D557 in LRR17 region from one monomer and amino acids Y356 in LRR11 domain and F408 in LRR13 domain from the second monomer together[5].

[2]Bam RA, Hansen D, et al. TLR7 Agonist GS-9620 Is a Potent Inhibitor of Acute HIV-1 Infection in Human Peripheral Blood Mononuclear Cells. Antimicrob Agents Chemother. 2017;61(1).

[3]Tsai A, Irrinki A, et al. Toll-Like Receptor 7 Agonist GS-9620 Induces HIV Expression and HIV-Specific Immunity in Cells from HIV-Infected Individuals on Suppressive Antiretroviral Therapy. J Virol. 2017;91(8).

[4]Lanford RE, Guerra B, 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;144(7):1508-17, 1517.e1-10.

[5]Rebbapragada I, Birkus G, et al. Molecular Determinants of GS-9620-Dependent TLR7 Activation. PLoS One. 2016;11(1):e0146835.

[6]Menne S, Tumas DB, et al. Sustained efficacy and seroconversion with the Toll-like receptor 7 agonist GS-9620 in the Woodchuck model of chronic hepatitis B. J Hepatol. 2015 Jun;62(6):1237-45.

[7]Gordon S. Pattern recognition receptors: doubling up for the innate immune response. Cell. 2002 Dec 27;111(7):927-30.

[8]Bam RA, Hansen D, Irrinki A, Mulato A, Jones GS, Hesselgesser J, Frey CR, Cihlar T, Yant SR. TLR7 Agonist GS-9620 Is a Potent Inhibitor of Acute HIV-1 Infection in Human Peripheral Blood Mononuclear Cells. Antimicrob Agents Chemother. 2016 Dec 27;61(1):e01369-16.

[9]Tsai A, Irrinki A, Kaur J, Cihlar T, Kukolj G, Sloan DD, Murry JP. Toll-Like Receptor 7 Agonist GS-9620 Induces HIV Expression and HIV-Specific Immunity in Cells from HIV-Infected Individuals on Suppressive Antiretroviral Therapy. J Virol. 2017 Mar 29;91(8):e02166-16.

[10]Lanford RE, Guerra B, Chavez D, Giavedoni L, Hodara VL, Brasky KM, Fosdick A, Frey CR, Zheng J, Wolfgang G, Halcomb RL, Tumas DB. GS-9620, an oral agonist of Toll-like receptor-7, induces prolonged suppression of hepatitis B virus in chronically infected chimpanzees. Gastroenterology. 2013 Jun;144(7):1508-17, 1517.e1-10.

[11]Rebbapragada I, Birkus G, Perry J, Xing W, Kwon H, Pflanz S. Molecular Determinants of GS-9620-Dependent TLR7 Activation. PLoS One. 2016 Jan 19;11(1):e0146835.

Vesatolimod/维沙莫德 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.18mL

2.44mL

1.22mL

24.36mL

4.87mL

2.44mL

Vesatolimod/维沙莫德 技术信息

CAS号1228585-88-3
分子式C22H30N6O2
分子量 410.51
SMILES Code O=C1NC2=C(N)N=C(OCCCC)N=C2N(CC3=CC=CC(CN4CCCC4)=C3)C1
MDL No. MFCD25372045
别名 GS-9620
运输蓝冰
InChI Key VFOKSTCIRGDTBR-UHFFFAOYSA-N
Pubchem ID 46241268
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

Tags: Vesatolimod | 1228585-88-3 | GS-9620 | GS9620 | GS 9620 | TLR7 Agonist | Immunology/Inflammation | Apoptosis | Anti-infection | Toll-like Receptor (TLR) | Apoptosis | HBV | HCV | HIV | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Vesatolimod/维沙莫德 纯度/质量文件 | Vesatolimod/维沙莫德 生物活性 | Vesatolimod/维沙莫德 动物研究 | Vesatolimod/维沙莫德 临床数据 | Vesatolimod/维沙莫德 参考文献 | Vesatolimod/维沙莫德 实验方案 | Vesatolimod/维沙莫德 技术信息

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