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Vesatolimod [1228585-88-3]

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Referentie NB-64-36274-5mg

Formaat : 5mg

Merk : Neo Biotech

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Vesatolimod

(Synonyms: GS-9620) Copy Product Info

Synonyms: GS-9620

Catalog No. T6846 Copy Product Info

Purity: 99.03%

Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7.

Cas No. 1228585-88-3

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.03%

Appearance:Solid

Color:White

Product Information

Bioactivity

Description	Vesatolimod (GS-9620) is an effective and specific orally active agonist of Toll-like receptor 7.
Targets & IC50	TLR7:291 nM(EC50)
In vitro	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].
In vivo	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.
Synonyms	GS-9620
Kinase Assay	Biochemical assays: Biochemical assays are performed by a broad-coverage, TR-FRET-based kinase binding assay platform.
Cell Research	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].

Chemical Properties

Molecular Weight	410.51
Formula	C₂₂H₃₀N₆O₂
Cas No.	1228585-88-3
Smiles	CCCCOc1nc(N)c2NC(=O)CN(Cc3cccc(CN4CCCC4)c3)c2n1
Relative Density.	1.247 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 35.71 mg/mL (86.99 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.57 mg/mL (8.7 mM), Solution.

10% DMSO+90% Saline: < 3.57 mg/mL (8.7 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4360 mL	12.1800 mL	24.3599 mL	121.7997 mL
5 mM	0.4872 mL	2.4360 mL	4.8720 mL	24.3599 mL
10 mM	0.2436 mL	1.2180 mL	2.4360 mL	12.1800 mL
20 mM	0.1218 mL	0.6090 mL	1.2180 mL	6.0900 mL
50 mM	0.0487 mL	0.2436 mL	0.4872 mL	2.4360 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.