TLR8 agonist 2 hydrochloride

Name: TLR8 agonist 2 hydrochloride
Brand: TargetMol
SKU: T40040
Rating: 4.5 (1 reviews)

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Catalog No. T40040Cas No. 2412937-65-4

TLR8 agonist 2 hydrochloride is a highly potent and selective agonist for human TLR8, with an EC50 of 3 nM, but demonstrates significantly weaker activity towards human TLR7 (EC50 of 33.33 μM).

TLR8 agonist 2 hydrochloride

😃Good

Catalog No. T40040Cas No. 2412937-65-4

TLR8 agonist 2 hydrochloride is a highly potent and selective agonist for human TLR8, with an EC50 of 3 nM, but demonstrates significantly weaker activity towards human TLR7 (EC50 of 33.33 μM).

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Product Introduction

Bioactivity

Description	TLR8 agonist 2 hydrochloride is a highly potent and selective agonist for human TLR8, with an EC50 of 3 nM, but demonstrates significantly weaker activity towards human TLR7 (EC50 of 33.33 μM).
Targets&IC50	TLR8:3 nM (EC50), TLR7:33.33 μM (EC50)
In vitro	TLR8 agonist 2 (Example 1) elevates TNF-α, IL-12p40, IFN-γ, and IFN-α levels in human peripheral blood mononuclear cells (hPBMC) with EC50 values of 105 nM, 26 nM, 29 nM, and 2800 nM, respectively[1].
In vivo	The pharmacokinetic parameters of TLR8 agonist 2 (Example 1) in mice administered intravenously at 1 mg/kg and orally at 5 mg/kg were evaluated. The T 1/2 of TLR8 agonist 2 were 0.25 h (1 mg/kg i.v.) and 0.5 h (5 mg/kg p.o.), with AUC last values of 450 ng/mLhr (i.v.) and 624 ng/mLhr (p.o.). The oral bioavailability (%F) was 27.7%[1].

Chemical Properties

Formula	C₁₆H₂₂N₈.xHCl
Cas No.	2412937-65-4
Smiles	N([C@@](CC=1NC=NN1)(CCCC)C)C=2C3=C(N=C(N)N2)C=NC=C3.Cl
Relative Density.	no data available

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.

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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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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.

Dose Conversion

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