| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
The primary molecular target of CAY10602 HCl is SIRT1 (sirtuin 1), a NAD(+)-dependent protein deacetylase. SIRT1 is a member of the sirtuin family of proteins that catalyze the deacetylation of lysine residues on histone and non-histone proteins in a NAD(+)-dependent manner. SIRT1 is involved in the regulation of various cellular processes, including metabolism, inflammation, apoptosis, and aging. By deacetylating transcription factors such as NF-κB and PPAR-γ, SIRT1 modulates the expression of genes involved in inflammation and metabolism. CAY10602 activates SIRT1, enhancing its deacetylase activity. This leads to increased deacetylation of SIRT1 substrates, including NF-κB, which suppresses NF-κB-dependent induction of TNF-α and other pro-inflammatory cytokines. The activation of SIRT1 by CAY10602 also promotes the deacetylation of PPAR-γ, which is involved in fatty acid metabolism and adipocyte differentiation. The compound's anti-obesity and antidiabetic properties are attributed to its effects on SIRT1-mediated metabolic regulation.
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| ln Vitro |
In vitro activity of CAY10602 HCl is characterized by its activation of SIRT1 and its anti-inflammatory and metabolic effects. In SIRT1 deacetylase assays using purified SIRT1 and a fluorogenic substrate, CAY10602 increases SIRT1 activity in a dose-dependent manner, with EC50 values in the low micromolar range. In cell-based assays, CAY10602 suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells in a dose-dependent manner. The compound also promotes the deacetylation of SIRT1 substrates, including NF-κB and PPAR-γ, as measured by Western blotting using acetylation-specific antibodies. In adipocyte differentiation assays, CAY10602 affects fat mobilization in differentiated adipocytes. The compound's effects on glucose metabolism and insulin sensitivity are assessed in various cell-based models. The compound's IC50 for inhibition of TNF-α production and EC50 for SIRT1 activation would be determined from dose-response curves.
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| ln Vivo |
In vivo activity of CAY10602 HCl has been demonstrated in animal models of inflammation, obesity, and diabetes. The compound's anti-obesity and antidiabetic properties have been reported. In models of obesity and diabetes, CAY10602 would be expected to improve metabolic parameters, including glucose tolerance, insulin sensitivity, and lipid profiles. In models of inflammation, the compound would be expected to reduce inflammatory cytokine levels and tissue inflammation through its activation of SIRT1 and suppression of NF-κB. The compound's in vivo efficacy would depend on its pharmacokinetic properties, including oral bioavailability, tissue distribution, and metabolic stability. Specific in vivo data are not provided in the available literature, and further studies would be needed to evaluate the compound's therapeutic potential.
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| Additional Infomation |
CAY10602 HCl (CAS# 374922-43-7) is a SIRT1 activator that suppresses NF-κB-dependent TNF-α induction and has anti-obesity and antidiabetic properties. Future research could focus on optimizing the compound's SIRT1 activation potency and selectivity, evaluating its in vivo efficacy in animal models of metabolic and inflammatory diseases, and developing it as a potential therapeutic for obesity, diabetes, and inflammatory disorders.
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| Appearance |
Typically exists as solid at room temperature
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| Synonyms |
CAY-10602 HCl; CAY 10602; CAY10602
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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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