| ln Vitro |
XL-3158 (compound XL-3158) (20 μM, 4 h) blocks intracellular aggregation of cGAS and DNA by inhibiting phase separation of cGAS in L929 cells [1]. XL-3158 (10-40 μM, 4 h) specifically inhibits downstream signaling activation of the cGAS-STING pathway in THP-1 Dual cells [1]. XL-3158 (10 μM, 4 h) selectively inhibits the DNA-triggered cGAS-dependent interferon pathway in THP-1 Dual cells [1]. XL-3158 (0-20 μM, 24 h) has a CC50 value of 77.55 μM for THP-1 cells and 56.79 μM for RAW-ISG cells [1].
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| ln Vivo |
XL-3158 (compound XL-3158) (25 mg/kg, administered twice by gavage) can alleviate secretin-induced acute pancreatitis [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: THP-1 Double-positive cells Tested Concentrations: 10 μM, 20 μM, 40 μM Incubation Duration: 4 hours Experimental Results: Inhibited HT-DNA-induced TBK-1 and IRF3 phosphorylation in a dose-dependent manner. No inhibitory effect on Poly(I:C) or cGAMP-activated signaling pathways. RT-PCR[1] Cell Types: THP-1 two-cell Tested Concentrations: 10 μM, 20 μM, 40 μM Incubation Duration: 4 hours Experimental Results: Significantly reduced HT-DNA-induced IFN-β1 mRNA expression. Immunofluorescence [1] Cell Types: L929 cells Tested Concentrations: 20 μM Incubation Duration: 4 hours Experimental Results: Significantly reduced the number of cGAS and Cy5-DNA colocalized aggregates. This confirmed that these aggregates possess liquid-phase separation (LLPS) properties and inhibited their formation. |
| Animal Protocol |
Animal/Disease Models:An acute pancreatitis model was induced in C57BL/6J nude mice (6-8 weeks old) using Cerulein (50 µg/kg, intraperitoneal injection, once per hour for 7 times) [1].
Doses: 25 mg/kg Route of Administration: Gavage (ig), administered 0 and 6 hours after the first Cerulein injection. Experimental Results: Significantly reduced pancreatic pathological damage and pancreas/body weight ratio, indicating relief of pancreatic edema. Significantly reduced serum amylase and serum lipase activities. Significantly reduced serum inflammatory factor levels. |
| References |
| CAS # |
3117797-77-7
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| Appearance |
Off-white to light yellow solid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 本产品在运输和储存过程中需避光（避免光照）。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~72.40 mM; with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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