| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
CBT-295 specifically targets and inhibits autotaxin (ATX) [2L24-L25, L29-L30]. By inhibiting ATX, CBT-295 reduces the production of lysophosphatidic acid (LPA), a signaling molecule involved in inflammation, cell proliferation, and fibrosis. This mechanism of action positions CBT-295 as a potential therapeutic for treating chronic liver diseases and the neuroinflammatory complications associated with hepatic encephalopathy [2L29-L32].
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| ln Vitro |
CBT-295 treatment results in a significant reduction in the levels of key pro-inflammatory cytokines, including transforming growth factor-beta (TGF-beta), tumor necrosis factor-alpha (TNF-alpha), and interleukin-6 (IL-6) in cell-based and tissue models [2L7-L9]. It also reduces the expression of the bile duct proliferation marker CK-19, indicating an effect on cholangiocyte proliferation [2L8-L9]. These in vitro data demonstrate the compound's potent anti-inflammatory and anti-fibrotic activity.
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| ln Vivo |
In a rat model of bile duct ligation (BDL)-induced chronic liver disease and hepatic encephalopathy, oral administration of CBT-295 (20 mg/kg, twice daily for 28 days) lowered liver fibrosis, as evidenced by reduced collagen deposition and improved liver function test parameters (ALT, AST, ALP) [2L7-L10, L42-L44]. Furthermore, CBT-295 reduced blood and brain ammonia levels and diminished neuroinflammation, characterized by a significant reduction in brain cytokine levels [2L10-L12, L31-L32].
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| Enzyme Assay |
The binding affinity of CBT-295 to autotaxin can be determined using a fluorescence-based enzymatic assay. Procedure: Purified human autotaxin (ATX) enzyme is incubated with varying concentrations of CBT-295 (e.g., 0.1 nM to 10 microM) in a 96-well black plate. The substrate (e.g., FS-3, a fluorogenic LPA analog) is added to initiate the reaction. After incubation at 37degC for 30-60 minutes, the fluorescence intensity is measured (excitation 485 nm, emission 530 nm). The IC50 value is calculated by plotting percent inhibition versus log inhibitor concentration using a non-linear regression analysis.
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| Cell Assay |
Anti-inflammatory activity can be assessed in primary macrophage cultures. Procedure: Bone marrow-derived macrophages are isolated from mice and seeded in 96-well plates. Cells are pre-treated with various concentrations of CBT-295 for 1 hour, then stimulated with lipopolysaccharide (LPS, 100 ng/mL) for 24 hours. Cell culture supernatants are collected, and the levels of pro-inflammatory cytokines (TNF-alpha, IL-6, IL-1beta, and TGF-beta) are quantified using commercial ELISA kits. Cytotoxicity is assessed using the MTT or LDH assay to ensure that observed cytokine reductions are not due to cell death.
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| Animal Protocol |
Chronic liver disease and hepatic encephalopathy rat model: Male Sprague-Dawley rats undergo bile duct ligation (BDL) surgery to induce chronic liver injury and secondary hepatic encephalopathy. One week post-surgery, rats are orally administered CBT-295 (20 mg/kg, twice daily) or vehicle control for 28 days. At the end of the treatment period, blood samples are collected for liver function tests (ALT, AST, ALP, albumin) and ammonia levels. Brain tissues are harvested for analysis of pro-inflammatory cytokines. Liver tissues are collected for histological analysis (collagen staining, CK-19 immunohistochemistry) to assess fibrosis and bile duct proliferation.
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| ADME/Pharmacokinetics |
As an orally active compound, CBT-295 is designed for oral administration [2L24-L25, L29-L30]. While specific PK parameters (t1/2, Cmax, AUC, oral bioavailability) are not detailed in the search results, the demonstrated in vivo efficacy in a 28-day oral dosing study at 20 mg/kg BID confirms that the compound has sufficient systemic exposure to exert its pharmacological effects. This suggests favorable absorption, distribution, metabolism, and excretion (ADME) properties following oral administration in rats.
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| Toxicity/Toxicokinetics |
Toxicology data for CBT-295 from the 28-day BDL rat study showed that the compound was tolerated at the tested dose of 20 mg/kg BID. The study did not report any overt signs of systemic toxicity or adverse effects on overall animal health, as indicated by the analysis of plasma samples for liver function (ALT, AST, ALP) and albumin levels [2L42-L44]. However, a comprehensive toxicological evaluation would be required for further development.
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| References | |
| Additional Infomation |
CBT-295 represents a potential therapeutic strategy for chronic liver disease and associated hepatic encephalopathy by targeting the ATX-LPA pathway [2L29-L32]. Activation of the ATX-LPA axis is implicated in liver fibrosis, neuroinflammation, and the pathogenesis of hepatic encephalopathy. By inhibiting ATX, CBT-295 reduces LPA production, leading to decreased inflammation and fibrosis. The research on CBT-295 highlights the therapeutic potential of ATX inhibitors for treating both the peripheral (liver) and central nervous system (CNS) complications of chronic liver disease. CBT-295 is a research-use only compound and is not yet an approved drug for human use.
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| Molecular Formula |
C18H20CLN3O
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| Molecular Weight |
329.82
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| Appearance |
White to off-white solid powder
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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: (1). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~151.60 mM; with ultrasonication)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0320 mL | 15.1598 mL | 30.3196 mL | |
| 5 mM | 0.6064 mL | 3.0320 mL | 6.0639 mL | |
| 10 mM | 0.3032 mL | 1.5160 mL | 3.0320 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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