CD 1530 |
Catalog No.GC11794
One-Click Copy Product Info
|
RAR receptor agonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 107430-66-0
Sample solution is provided at 25 µL, 10mM.
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Target: RARγ, RARβ and RARα
Ki: 150, 1500, and 2750 nM
CD1530 is a potent and selective RAR receptor agonist with Ki values of 150, 1500 and 2750 nM for RARγ, RARβ and RARα receptors, respectively [1]. In addition, CD1530 shows moderate RARγ selectivity in the transcriptional assay with AC50 value of 1.8 nM. RAR-α is present in the majority of tissues while the distribution of RAR-β and γ is more selective [1]. RARγ mediated retinoic acid (RA)-induced growth arrest and apoptosis of neoplastic mouse papilloma cell lines [2].
In vitro: CD1530 inhibited excessive ROS production in tongue epithelial cells [2]. In addition, CD1530 was also a potent CYP26A1 inhibitor as ketoconazole with an IC50 value of 530 nM [3].
In vivo: The combination of the drugs bexarotene (300 mg/kg) and CD1530 (2.5 mg/100 mL in drinking water) was more effective than either drug alone in preventing oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide (4-NQO) in a mouse model of oral-cavity squamous-cell carcinoma (OCSCC), which did not cause cardiovascular risks [2]. High fat diet (HFD)-fed mice treated with CD1530 (2.5 mg/100 ml in drinking water) showed no decreases in steatosis, Kupffer cell TGF-β1 expression, or Hepatic stellate cells (HSCs) activation [4].
References:
1. Thacher SM, Vasudevan J, Chandraratna RA. Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000;6(1):25-58.
2. 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;111(24):8907-12.
3. Thatcher JE, Buttrick B, Shaffer SA, Shimshoni JA, Goodlett DR, Nelson WL, et al. Substrate specificity and ligand interactions of CYP26A1, the human liver retinoic acid hydroxylase. Mol Pharmacol. 2011;80(2):228-39.
4. Trasino SE, Tang XH, Jessurun J, Gudas LJ. A retinoic acid receptor beta2 agonist reduces hepatic stellate cell activation in nonalcoholic fatty liver disease. J Mol Med (Berl). 2016.
| Cas No. | 107430-66-0 | SDF | |
| Chemical Name | 4-(7-((1s,3R,5S,7s)-adamantan-1-yl)-6-hydroxynaphthalen-2-yl)benzoic acid | ||
| Canonical SMILES | OC1=CC2=CC=C(C3=CC=C(C(O)=O)C=C3)C=C2C=C1[C@]4(C[C@H]5C6)C[C@@H](C5)C[C@H]6C4 | ||
| Formula | C27H26O3 | M.Wt | 398.49 |
| Solubility | 50 mM in 1 eq. NaOH: Soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5095 mL | 12.5474 mL | 25.0947 mL |
| 5 mM | 501.9 μL | 2.5095 mL | 5.0189 mL |
| 10 mM | 250.9 μL | 1.2547 mL | 2.5095 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)