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| 25mg |
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Purity: ≥98%
CAY 10465, an analog of resveratrol, is a novel, potent, selective and high-affinityAhR (aryl hydrocarbon receptor) agonist, with aKiof 0.2 nM, and shows no effect on estrogen receptor (Ki>100000 nM).
| Targets |
CAY 10465 (Compound 4i) is a high-affinity, selective agonist for the AhR receptor with a Ki of 0.2 nM. It has no impact on the estrogen receptor (Ki >100000 nM) [1]. In HepG2 cells, CAY 10465 (0.01 nM-100 μM) decreases apolipoprotein AI (apo AI) levels and prevents this protein from being synthesized [2].
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| ln Vitro |
CAY 10465 (Compound 4i) is a high-affinity, selective agonist for the AhR receptor with a Ki of 0.2 nM. It has no impact on the estrogen receptor (Ki >100000 nM) [1]. In HepG2 cells, CAY 10465 (0.01 nM-100 μM) decreases apolipoprotein AI (apo AI) levels and prevents this protein from being synthesized [2].
Treatment of HepG2 cells with CAY10465 (0.1 nM to 100 μM) for 24 hours inhibited apolipoprotein A-I (apo A-I) protein secretion in a dose-dependent manner, with significant inhibition observed at concentrations ≥100 nM[2] CAY10465 (100 nM) increased cytochrome P450 1A1 (CYP1A1) mRNA expression 2.6-fold in HepG2 cells after 24 hours, an effect reversed by co-treatment with the AhR antagonist CAY10464[2] |
| Cell Assay |
HepG2 cells were maintained in Dulbecco’s Modified Essential Medium containing 10% fetal bovine serum and antibiotics. Cells were treated with CAY10465 at indicated concentrations for 24 hours. Apo A-I protein levels in conditioned medium were measured by Western blot using anti-human apo A-I antibody[2]
For mRNA analysis, HepG2 cells were treated with CAY10465 for 24 hours. Total RNA was isolated, reverse transcribed, and quantitative real-time PCR was performed using primers for CYP1A1 and GAPDH. CYP1A1 mRNA levels were normalized to GAPDH[2] |
| References |
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| Additional Infomation |
CAY10465 is a stilbene derivative of resveratrol that acts as an aryl hydrocarbon receptor (AhR) agonist.[2]
Its structure differs from benzo[a]pyrene, but it can also bind to AhR and exhibits functional activity in inhibiting the expression of apolipoprotein AI (apo AI) in hepatocytes.[2] CAY10465 was used as a tool compound to demonstrate that AhR activation inhibits apo AI gene expression, suggesting a mechanism of smoking-induced hypoalphalipoproteinemia.[2] |
| Molecular Formula |
C₁₅H₉CL₂F₃
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|---|---|
| Molecular Weight |
317.13
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| Exact Mass |
316.003
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| Elemental Analysis |
C, 56.81; H, 2.86; Cl, 22.36; F, 17.97
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| CAS # |
688348-33-6
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| PubChem CID |
11438491
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
361.2±42.0 °C at 760 mmHg
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| Flash Point |
201.8±21.3 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.597
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| LogP |
7.01
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
323
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1=CC=C(/C=C/C2=CC(Cl)=CC(Cl)=C2)C=C1)(F)F
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| InChi Key |
ISPYNXGXZRLLHM-OWOJBTEDSA-N
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| InChi Code |
InChI=1S/C15H9Cl2F3/c16-13-7-11(8-14(17)9-13)2-1-10-3-5-12(6-4-10)15(18,19)20/h1-9H/b2-1+
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| Chemical Name |
1,3-dichloro-5-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]benzene
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| Synonyms |
CAY 10465;CAY10465;CAY-10465
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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) |
DMSO: 10 mM
Water:N/A
Ethanol:N/A
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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 | 3.1533 mL | 15.7664 mL | 31.5328 mL | |
| 5 mM | 0.6307 mL | 3.1533 mL | 6.3066 mL | |
| 10 mM | 0.3153 mL | 1.5766 mL | 3.1533 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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