| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 250mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
RARγ (retinoic acid receptor gamma). CD-1530 is a potent and selective RARγ agonist. It binds to RARγ with high affinity, exhibiting a Ki value of 150 nM. It is more than 10-fold selective for RARγ over RARβ and RARα, with Ki values of 1500 nM and 2750 nM, respectively. By binding to RARγ, CD-1530 activates the receptor, leading to the modulation of transcription of target genes involved in cell differentiation, proliferation, and apoptosis.
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| ln Vitro |
In vitro, CD-1530 is a selective and potent RARγ agonist. It activates RARγ-mediated transcriptional activity with an AC50 of 1.8 nM. It displays high affinity for RARγ with a Kd of 150 nM. CD-1530 has been shown to have potential anticancer activity in vitro. It is also a potent inhibitor of CYP26A1, with an IC50 of 530 nM, comparable to ketoconazole.
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| ln Vivo |
CD-1530 has demonstrated in vivo efficacy in several preclinical models. It facilitates Achilles tendon healing by modulating the healing environment and reducing chondrification in a mouse model. In a murine model of oral cavity carcinogenesis, CD-1530 has been shown to substantively reduce the numbers of carcinomas that develop. It has been used in combination with bexarotene to inhibit oral carcinogenesis induced by 4-nitroquinoline 1-oxide in mouse models.
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| Enzyme Assay |
The activity of CD-1530 as a selective RARγ agonist is typically assessed using in vitro radioligand binding assays to measure its affinity for RARγ, RARβ, and RARα receptors. These assays determine the Ki values for each receptor subtype. Additionally, functional assays, such as reporter gene assays, are used to measure the compound's ability to activate RARγ-mediated transcriptional activity, from which an AC50 value is derived.
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| Cell Assay |
Cellular assays for CD-1530 involve treating cells with the compound and measuring RARγ-mediated transcriptional activity. This is commonly done using reporter gene assays, where cells are transfected with a luciferase reporter construct driven by RAR response elements. The compound's effects on cell proliferation, differentiation, and gene expression are also evaluated in various cell types to study its biological activity.
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| Animal Protocol |
In vivo animal model protocols for CD-1530 involve its administration to mouse models of disease. In a mouse Achilles tendon rupture model, local injection of CD-1530 was used to facilitate histological tendon healing. In a murine model of oral cavity carcinogenesis, the compound was administered to evaluate its chemopreventive effects. Specific dosing regimens and routes of administration vary depending on the disease model being studied.
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| ADME/Pharmacokinetics |
CD-1530 has a molecular weight of 398.49 and a molecular formula of C₂₇H₂₆O₃. Its CAS number is 107430-66-0. It is soluble in DMSO. The compound is typically stored at +4°C or at -20°C for long-term stability. Specific pharmacokinetic data, such as half-life and bioavailability, is not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Specific toxicological data for CD-1530 is not extensively detailed in the available literature. As a research compound, it is intended for research use only and not for human consumption. Standard safety assessments would be required for clinical development. The compound has shown insecticidal activity against Cryptobacterium hidradii nematodes.
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| References |
: Tang XH, Osei-Sarfo K, Urvalek AM, Zhang T, Scognamiglio T, Gudas LJ. Combination of bexarotene and the retinoid CD1530 reduces murine oral-cavity carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide. Proc Natl Acad Sci U S A. 2014 Jun 17;111(24):8907-12. doi: 10.1073/pnas.1404828111. Epub 2014 Jun 3. PubMed PMID: 24927566; PubMed Central PMCID: PMC4066471.
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| Additional Infomation |
CD-1530 (CAS# 107430-66-0) is a research compound used to study RARγ function. It is a selective and potent RARγ agonist with potential anticancer activity. It has been investigated for its therapeutic potential in tendon healing and for the chemoprevention of oral and esophageal squamous cell carcinoma. It is not approved for clinical use and is supplied as a research chemical.
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| Molecular Formula |
C27H26O3
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|---|---|
| Molecular Weight |
398.49354
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| Exact Mass |
398.188
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| CAS # |
107430-66-0
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| Related CAS # |
107430-66-0
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| PubChem CID |
9952709
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| Appearance |
Light brown to brown solid powder
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| Density |
1.29g/cm3
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| Boiling Point |
610.7ºC at 760 mmHg
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| Flash Point |
337.2ºC
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| Vapour Pressure |
9.03E-16mmHg at 25°C
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| Index of Refraction |
1.688
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| LogP |
6.378
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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 |
30
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| Complexity |
622
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O)C1=CC=C(C2=CC=C3C=C(O)C(C4(C5)CC6CC5CC(C6)C4)=CC3=C2)C=C1
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| InChi Key |
VCQGNUWOMLYNNG-PSAKPEQJSA-N
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| InChi Code |
InChI=1S/C27H26O3/c28-25-12-22-6-5-21(19-1-3-20(4-2-19)26(29)30)10-23(22)11-24(25)27-13-16-7-17(14-27)9-18(8-16)15-27/h1-6,10-12,16-18,28H,7-9,13-15H2,(H,29,30)/t16-,17+,18-,27?
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| Chemical Name |
4-(7-((3r,5r,7r)-adamantan-1-yl)-6-hydroxynaphthalen-2-yl)benzoic acid
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| Synonyms |
CD1530 CD 1530 CD-1530.
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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 : ~100 mg/mL (~250.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5095 mL | 12.5474 mL | 25.0947 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL | |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5095 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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