Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

GSK717 [1595278-21-9]

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Cat# NB-64-26109-1mL

Size : 1mLx10mM(inDMSO)

Marca : Neo Biotech

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GSK717

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Synonyms:

Catalog No. T38361 Copy Product Info

Purity: 99.01%

GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor that inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling with an IC₅₀ of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1]. It blocks the synergy between NOD2 and TLR2 without affecting NOD1, TNFR1, and TLR2-mediated responses. At 5 μM, GSK717 inhibits the release of IL-8, IL-6, TNFα, and IL-1β in primary human monocytes stimulated with MDP[1].

[1]. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.

Cas No. 1595278-21-9

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

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Purity:99.01%

Appearance:Solid

Color:White

Product Information

Bioactivity

Description	GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor that inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling with an IC₅₀ of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1]. It blocks the synergy between NOD2 and TLR2 without affecting NOD1, TNFR1, and TLR2-mediated responses. At 5 μM, GSK717 inhibits the release of IL-8, IL-6, TNFα, and IL-1β in primary human monocytes stimulated with MDP[1]. [1]. Rickard DJ, et al. Identification of benzimidazole diamides as selective inhibitors of the nucleotide-binding oligomerization domain 2 (NOD2) signaling pathway. PLoS One. 2013;8(8):e69619. Published 2013 Aug 1.
In vitro	GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells[1].

Chemical Properties

Molecular Weight	452.55
Formula	C₂₈H₂₈N₄O₂
Cas No.	1595278-21-9
Smiles	CN(CCc1nc2ccccc2n1CC(=O)Nc1ccc2CCCc2c1)C(=O)c1ccccc1
Relative Density.	1.23 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 135 mg/mL (298.31 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Saline: < 10 mg/mL (22.1 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (22.1 mM), Solution.

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	2.2097 mL	11.0485 mL	22.0970 mL	110.4850 mL
5 mM	0.4419 mL	2.2097 mL	4.4194 mL	22.0970 mL
10 mM	0.2210 mL	1.1049 mL	2.2097 mL	11.0485 mL
20 mM	0.1105 mL	0.5524 mL	1.1049 mL	5.5243 mL
50 mM	0.0442 mL	0.2210 mL	0.4419 mL	2.2097 mL
100 mM	0.0221 mL	0.1105 mL	0.2210 mL	1.1049 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.

Dose Conversion

Keywords

synergyresponsespro-inflammatoryNOD-like Receptor (NLR)NOD2-TLR2NOD2MDP-stimulatedInhibitorinhibitimmuneILReceptorIL-8IL ReceptorGSK-717GSK717GSK 717cytokines

Related Tags: GSK717 chemical structure | GSK717 in vitro | GSK717 formula | GSK717 molecular weight