Product Details
| Product Name:
Vesatolimod |
CAS No.:
1228585-88-3 |
| Purity:
99.92% |
Supply Ability:
10g |
| Release date:
2024/11/14 |
Product Introduction
Bioactivity
| 名稱 | Vesatolimod |
| 描述 | Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7. |
| 細(xì)胞實(shí)驗(yàn) | GS-9620 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Daudi cells are incubated for indicated times with varying concentrations [3H]GS-9620 (0.7μCi/mL). Cell associated radioactivity is extracted with ice cold 80% ethanol and measured using liquid scintillation counting. The total amount of GS-9620 in cells is calculated from a calibration curve for GS-9620 mass versus radioactivity. Cell volume is measured[1]. |
| 激酶實(shí)驗(yàn) | Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform. |
| 體外活性 | Vesatolimod rapidly internalizes into cells and preferentially localizes to and signals from endo-lysosomal compartments. To test this hypothesis, the kinetics of cellular uptake of the compound in Daudi cells using tritiated Vesatolimod (3H-Vesatolimod) is measured. The kinetics of 3H-Vesatolimod accumulation is rapid, reaching concentration-dependent steady-state equilibrium in approximately thirty minutes. Measured intracellular concentration of 3H-Vesatolimod is 5-fold higher than the extracellular concentration of 3H-Vesatolimod used to treat cells. Increases in intracellular 3H-Vesatolimod concentrations are roughly proportional with increasing concentrations of 3H-Vesatolimod[1]. |
| 體內(nèi)活性 | Administering single oral doses of GS-9620 at 0.3 and 1 mg/kg to uninfected chimpanzees resulted in a dose-dependent increase in serum interferon alpha (IFN-α), various cytokines/chemokines, and activation of interferon-stimulated genes (ISG) in both peripheral blood and liver tissues. Specifically, GS-9620 reached peak plasma concentrations (Cmax) of 3.6±3.5 nM at 0.3 mg/kg (n=3), 36.8±34.5 nM at 1 mg/kg (n=3), and 55.4±81.0 nM at 1 mg/kg (n=4), respectively, with peak serum interferon responses recorded 8 hours after dosing. The induced peak serum levels of IFN-α were measured at 66 pg/mL for the 0.3 mg/kg dose and 479 pg/mL for the 1 mg/kg dose. Treatment with GS-9620 at these doses also elevated ISG transcripts, specifically ISG15, OAS-1, MX1, IP-10 (CXCL10), and I-TAC (CXCL11), in peripheral blood mononuclear cells (PBMC) at the lower dose and in both PBMC and liver at the higher dose. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 4.1 mg/mL (10 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Hepatitis B virus | HCV | inhibit | Vesatolimod | Apoptosis | Human immunodeficiency virus | GS9620 | Inhibitor | HBV | Hepatitis C virus | HIV | GS 9620 | Toll-like Receptor (TLR) |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Emtricitabine | Sodium 4-phenylbutyrate | L-Ascorbic acid | Hydroxychloroquine | Lamivudine | Tributyrin |
| 相關(guān)庫(kù) | 細(xì)胞重編程化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 膜蛋白靶向化合物庫(kù) | ReFRAME 相關(guān)化合物庫(kù) | 細(xì)胞焦亡化合物庫(kù) | 抗病毒庫(kù) | 藥物功能重定位化合物庫(kù) | 臨床期小分子藥物庫(kù) | 已知活性化合物庫(kù) | 抗COVID-19化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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