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XL-3158
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Catalog No. T210767
XL-3158 is an orally active inhibitor of cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) with human cGAS IC50 of 11.1 μM and murine cGAS IC50 of 2.19 μM. It binds both allosteric and orthosteric sites, stabilizing the inactive closed conformation of the enzyme, thereby weakening cGAS interaction with DNA. By targeting phase separation, XL-3158 effectively penetrates cells, reduces intracellular cGAS local concentration through inhibition of aggregate formation, and shows no significant cytotoxicity at effective concentrations, making it suitable for subsequent cellular function experiments. XL-3158 overcomes species selectivity barriers, presenting a candidate drug for cGAS-dependent inflammatory diseases.
XL-3158
XL-3158
Copy Product Info😃Good
Catalog No. T210767
XL-3158 is an orally active inhibitor of cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) with human cGAS IC50 of 11.1 μM and murine cGAS IC50 of 2.19 μM. It binds both allosteric and orthosteric sites, stabilizing the inactive closed conformation of the enzyme, thereby weakening cGAS interaction with DNA. By targeting phase separation, XL-3158 effectively penetrates cells, reduces intracellular cGAS local concentration through inhibition of aggregate formation, and shows no significant cytotoxicity at effective concentrations, making it suitable for subsequent cellular function experiments. XL-3158 overcomes species selectivity barriers, presenting a candidate drug for cGAS-dependent inflammatory diseases.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | XL-3158 is an orally active inhibitor of cyclic guanosine monophosphate-adenosine monophosphate synthase (cGAS) with human cGAS IC50 of 11.1 μM and murine cGAS IC50 of 2.19 μM. It binds both allosteric and orthosteric sites, stabilizing the inactive closed conformation of the enzyme, thereby weakening cGAS interaction with DNA. By targeting phase separation, XL-3158 effectively penetrates cells, reduces intracellular cGAS local concentration through inhibition of aggregate formation, and shows no significant cytotoxicity at effective concentrations, making it suitable for subsequent cellular function experiments. XL-3158 overcomes species selectivity barriers, presenting a candidate drug for cGAS-dependent inflammatory diseases. |
| In vitro | XL-3158 (Compound XL-3158) at a concentration of 20 μM for 4 hours inhibits phase separation of cGAS in L929 cells, thereby preventing intracellular condensation of cGAS with DNA. At concentrations ranging from 10-40 μM, administered for 4 hours, XL-3158 specifically blocks downstream signaling activation of the cGAS-STING pathway in THP-1 Dual cells. When applied at 10 μM for 4 hours, it selectively suppresses the DNA-triggered cGAS-dependent interferon pathway in THP-1 Dual cells. The compound has a CC50 of 77.55 μM in THP-1 cells and 56.79 μM in RAW-ISG cells when used in the range of 0-20 μM for 24 hours. |
| In vivo | XL-3158 (Compound XL-3158) administered at 25 mg/kg through intragastric route twice, significantly alleviates acute pancreatitis. It exhibits favorable oral bioavailability and in vivo activity, supporting its potential as a candidate drug for cGAS-dependent inflammatory diseases. |
| 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, 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.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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