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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
😃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
| 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 & 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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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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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