| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
CD 3159 targets retinoid X receptors (RXRs), which play a central role in regulating intracellular receptor signaling pathways. It acts as an antagonist toward RXR homodimers but functions as an agonist when RXR is paired as a heterodimer with PPARα or PPARγ. This dimer-selective ligand confers differential interactions on the transcription machinery.
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| ln Vitro |
One specific activator of endogenous RXR heterodimers is LG100754 [1]. In mature adipocytes, TNFα-mediated insulin resistance can also be ameliorated by LG100754 [1]. Genuine activation of the endogenous RXR:PPARγ heterodimer and modulation of insulin-dependent signaling pathways are exhibited by LG100754 [1].
In vitro, CD 3159 (LG 100754) has minimal intrinsic transcriptional activity but enhances the potency of PPARγ-RXR heterodimers for PPARγ ligands. It sensitizes cells to low concentrations of PPARγ ligands. The compound demonstrates antidiabetic properties in cell-based reporter assays measuring PPARγ-RXR heterodimer activation. |
| ln Vivo |
The fact that LG100754 (100 mg/kg) totally prevents the rise in glucose levels suggests that LG100754 can help the body become more insulin resistant [1].
In vivo, CD 3159 decreases glucose levels and relieves insulin resistance in mouse models. It demonstrates antidiabetic properties in vivo by enhancing insulin sensitivity through PPARγ-RXR heterodimer activation. |
| Enzyme Assay |
In vitro receptor binding assays for RXR ligands typically use radioligand binding with [³H]9-cis-retinoic acid as the labeled ligand. Membranes prepared from cells expressing RXR are incubated with the radioligand and varying concentrations of CD 3159. Specific binding is determined by subtracting non-specific binding. IC50 or Ki values are calculated from competition binding curves.
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| Cell Assay |
In vitro cellular assays typically use reporter gene assays in cells transfected with RXR, PPARγ, and a luciferase reporter construct. Cells are treated with CD 3159 at various concentrations, and luciferase activity is measured after 16-24 hours. The compound's ability to enhance PPARγ ligand potency is assessed by measuring the shift in EC50 of PPARγ agonists.
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| Animal Protocol |
In vivo animal studies for antidiabetic efficacy typically use mouse models of insulin resistance or type 2 diabetes. Animals are administered CD 3159 orally at various doses for a defined treatment period. Blood glucose levels are measured, and insulin tolerance tests (ITT) are performed. The compound's ability to relieve insulin resistance and decrease glucose levels is assessed.
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| ADME/Pharmacokinetics |
CD 3159 is orally bioavailable with good absorption following oral administration. As a lipophilic RXR ligand, it distributes to tissues expressing RXRs. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys and bile. Detailed PK parameters are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CD 3159 would typically include acute and repeated-dose toxicity in rodents, as well as genotoxicity and safety pharmacology assessments. As an RXR ligand, potential effects on lipid metabolism and thyroid function should be monitored. The compound is generally well-tolerated at therapeutic doses.
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| References | |
| Additional Infomation |
CD 3159 (LG 100754) is a dimer-selective RXR ligand that acts as an antagonist of RXR homodimers but an agonist of RXR:PPARα and RXR:PPARγ heterodimers. It is an insulin sensitizer that decreases glucose levels and relieves insulin resistance. The compound is available for research use only and is not approved for clinical use.
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| Molecular Formula |
C26H36O3
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|---|---|
| Molecular Weight |
396.57
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| Exact Mass |
396.266
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| CAS # |
180713-37-5
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| PubChem CID |
6442223
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| Appearance |
White to off-white solid powder
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| Density |
1.003g/cm3
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| Boiling Point |
549.4ºC at 760 mmHg
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| Flash Point |
178.5ºC
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| Vapour Pressure |
6.63E-13mmHg at 25°C
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| Index of Refraction |
1.526
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| LogP |
6.814
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
29
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| Complexity |
665
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCOC1=CC2=C(C=C1/C(=C\C=C\C(=C\C(=O)O)\C)/C)C(CCC2(C)C)(C)C
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| InChi Key |
HNODNXQAYXJFMQ-LQUSFLDPSA-N
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| InChi Code |
InChI=1S/C26H36O3/c1-8-14-29-23-17-22-21(25(4,5)12-13-26(22,6)7)16-20(23)19(3)11-9-10-18(2)15-24(27)28/h9-11,15-17H,8,12-14H2,1-7H3,(H,27,28)/b10-9+,18-15+,19-11-
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| Chemical Name |
(2E,4E,6Z)-3-methyl-7-(5,5,8,8-tetramethyl-3-propoxy-6,7-dihydronaphthalen-2-yl)octa-2,4,6-trienoic acid
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| Synonyms |
LG100754 UVI2112 CD3159 LG-100754 CD-3159 UVI-2112 CD-3159 CD 3159
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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 (~252.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.30 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5216 mL | 12.6081 mL | 25.2162 mL | |
| 5 mM | 0.5043 mL | 2.5216 mL | 5.0432 mL | |
| 10 mM | 0.2522 mL | 1.2608 mL | 2.5216 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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