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| 5mg |
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| Targets |
CD3254 targets the retinoid X receptor (RXR), a nuclear receptor that forms heterodimers with other nuclear receptors such as RAR, PPAR, and VDR. As a selective RXR agonist, it binds to and activates RXR, modulating the transcription of target genes involved in cell differentiation, metabolism, and survival. CD3254 is a potent and selective RXR agonist.
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| ln Vitro |
After five days of exposure at low doses (20 μg/L) and one day at high concentrations (50 and 100 μg/L), CD3254 causes identical model abnormalities [1].
In vitro, CD3254 acts as a selective and potent RXR agonist. It has been shown to inhibit neuronal cell death under conditions of oxygen-glucose deprivation and reoxygenation. Exposure to CD3254 at concentrations of 20-100 μg/L induces phenotypic changes in cells. The compound's activity in modulating RXR-mediated transcription is well-characterized. |
| ln Vivo |
Specific in vivo activity data for CD3254 is not extensively detailed in the available literature. As a synthetic rexinoid, it is used to study RXR-dependent gene regulation and metabolic control. Its ability to inhibit neuronal cell death suggests potential neuroprotective effects in vivo. Further studies are needed to fully characterize its in vivo efficacy.
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| Enzyme Assay |
CD3254's activity as an RXR agonist is assessed using in vitro receptor binding assays to measure its affinity for RXR. These assays typically involve radioligand binding or fluorescence-based techniques to determine the compound's binding affinity and selectivity. Functional assays, such as reporter gene assays, are used to measure RXR-mediated transcriptional activity.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: zebrafish (Danio rerio) Embryonic Tested Concentrations: 10, 20, 50, 100 μg/L Incubation Duration: Experimental Results: Survival of 100 μg/L CD3254 treated group after day 1 exposure The rate diminished by 19.1%. Embryos did not hatch in the groups exposed to 100 μg/L CD3254 for 5 days or the first day of exposure to 1 mg/L CD3254. Cellular assays for CD3254 involve treating cells with the compound and measuring RXR-mediated transcriptional activity. Reporter gene assays, where cells are transfected with an RXR-responsive luciferase reporter, are commonly used. The compound's effects on cell differentiation, survival, and gene expression are also evaluated in various cell types. |
| Animal Protocol |
In vivo animal model protocols for CD3254 would involve its administration to animal models to study RXR-dependent processes. Studies may include models of neurodegeneration, metabolic disorders, or cancer to evaluate the compound's efficacy in modulating RXR-mediated pathways. Specific protocols would depend on the disease model being investigated.
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| ADME/Pharmacokinetics |
CD3254 has a molecular weight of 364.48 and a molecular formula of C24H28O3. It is soluble in DMSO (100 mg/mL) and ethanol (100 mM). The compound is supplied as a solid and should be stored at low temperature. Its lipophilic nature suggests good cell permeability.
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| Toxicity/Toxicokinetics |
CD3254 is intended for research use only and not for human consumption. As a research compound, its comprehensive toxicological profile may not be fully characterized. However, as a synthetic rexinoid, its safety profile would need to be evaluated in appropriate toxicology studies for clinical development.
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| References | |
| Additional Infomation |
Structure in the first source
CD3254 (CAS# 196961-43-0) is a research compound used to study retinoid X receptor (RXR) function. It is a selective and potent RXR agonist that modulates RXR-mediated transcriptional activity. It is used as a research tool to explore RXR-dependent gene regulation, cell differentiation, and metabolic control. It is not approved for clinical use. |
| Molecular Formula |
C24H28O3
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|---|---|
| Molecular Weight |
364.49
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| Exact Mass |
364.204
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| CAS # |
196961-43-0
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| PubChem CID |
44566110
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| Appearance |
White to yellow solid powder
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| LogP |
5.814
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
576
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(C=C1C3=C(C=CC(=C3)/C=C/C(=O)O)O)C(CCC2(C)C)(C)C
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| InChi Key |
DYLLZSVPAUUSSB-VQHVLOKHSA-N
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| InChi Code |
InChI=1S/C24H28O3/c1-15-12-19-20(24(4,5)11-10-23(19,2)3)14-17(15)18-13-16(6-8-21(18)25)7-9-22(26)27/h6-9,12-14,25H,10-11H2,1-5H3,(H,26,27)/b9-7+
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| Chemical Name |
(E)-3-[4-hydroxy-3-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)phenyl]prop-2-enoic acid
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| Synonyms |
CD-3254; CD 3254; CD3254
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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 : ~125 mg/mL (~342.95 mM)
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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 | 2.7436 mL | 13.7178 mL | 27.4356 mL | |
| 5 mM | 0.5487 mL | 2.7436 mL | 5.4871 mL | |
| 10 mM | 0.2744 mL | 1.3718 mL | 2.7436 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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