| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
IC50: LXR[1]
DMHCA targets liver X receptors (LXR), functioning as a selective LXR agonist. LXRs are nuclear receptors that play a central role in cholesterol metabolism, lipid homeostasis, and inflammation. By activating LXR, DMHCA promotes the expression of ATP-binding cassette (ABC) transporters involved in cholesterol efflux, such as ABCA1. It also upregulates FASN and SREBP-1alpha gene expression. The compound's anti-inflammatory effects and ability to modulate cholesterol homeostasis make it a valuable tool for studying LXR biology and developing therapeutic strategies for metabolic and inflammatory diseases. |
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| ln Vitro |
DMHCA (10 µM; 16–18 hours) treats diabetes CD34+ cells ex vivo and returns membrane fluidity to pre-diabetic levels[1]. When compared to control mice, DMHCA markedly reduces CCL-2 generation by >50% in the BM supernatants and the systemic circulation while restoring baseline levels of BM-derived TNF-α and IL-3. Additionally, DMHCA upregulates the egression of vascular reparative cells into the peripheral circulation and increases the amount of CACs in the BM and peripheral circulation [1]. According to the PAGA analysis, erythrocyte progenitor robustness and overall production are improved by DMHCA treatment. Flux down the erythrocyte progenitor lineage is improved by DMHCA. Moreover, it DMHCA raises the density of erythrocyte progenitor cells in bone marrow. DMHCA raises the expression of the hemoglobin beta adult chain (HBB-BT) in addition to increasing the fraction of erythrocyte progenitors[1].
In vitro, DMHCA demonstrates selective LXR agonist activity. It induces ABCA1 expression, promoting cholesterol efflux from cells. The compound upregulates FASN and SREBP-1alpha gene expression, indicating effects on lipid metabolism. DMHCA has anti-inflammatory effects, as assessed by measuring the production of inflammatory mediators in relevant cell models. It significantly increases endogenous LXR ligands, desmosterol, and total oxysterols. The compound's activity is typically assessed in cell-based reporter assays using LXR response element (LXRE)-luciferase constructs and by measuring the expression of LXR target genes such as ABCA1 by qPCR. |
| ln Vivo |
In diabetic retinal patients, DMHCA (oral dosage; 6 months; meal 8 mg/kg body weight /day) restores cholesterol homeostasis. In the diabetic retina, it markedly raises total oxysterol, desmosterol, and endogenous LXR ligands[1].
Specific in vivo activity data for DMHCA are limited in the publicly available literature. The compound has been studied in the context of cholesterol homeostasis and diabetes. It significantly increases endogenous LXR ligands, desmosterol, and total oxysterols in the diabetic retina. DMHCA may serve as a therapeutic agent for treating atherosclerosis, age-related macular degeneration, and diabetic retinopathy. Further in vivo studies are needed to fully characterize its efficacy and safety in these disease models. The compound's LXR agonist activity suggests potential applications in metabolic and inflammatory diseases. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for DMHCA typically involve competitive binding experiments using LXR proteins and radiolabeled or fluorescently labeled LXR ligands as tracers. The compound's binding affinity to LXR is assessed, with IC₅₀ or Kd values determined. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations. The compound's agonist activity is confirmed through functional assays measuring LXR-mediated transcriptional activation using LXRE-luciferase reporter constructs. Binding affinity and potency are expressed as IC₅₀ and EC₅₀ values.
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| Cell Assay |
In vitro cell-based assays for DMHCA utilize cell lines expressing LXR to assess its agonist activity. Cells are treated with varying concentrations of the compound for 24-48 hours. LXR-mediated transcriptional activity is evaluated using reporter gene assays with LXRE-luciferase constructs. The expression of LXR target genes such as ABCA1, FASN, and SREBP-1alpha is measured by qPCR. Cholesterol efflux assays can be used to assess the functional activity of ABCA1 induction. Anti-inflammatory activity is assessed by measuring the production of inflammatory cytokines. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed.
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| Animal Protocol |
In vivo animal studies with DMHCA would typically involve administration of the compound to rodent models of metabolic or inflammatory diseases. Potential study designs include models of atherosclerosis, diabetes, age-related macular degeneration, and diabetic retinopathy. Typical endpoints would include measurements of cholesterol levels, assessment of lipid metabolism, evaluation of inflammatory markers, and pharmacokinetic profiling. The compound's effects on LXR ligand levels and oxysterol profiles in target tissues can also be assessed. All procedures must comply with institutional animal care and use guidelines.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for DMHCA are not extensively documented in the publicly available literature. The compound has a molecular weight of 401.63 g/mol and a molecular formula of C₂₆H₄₃NO₂. It has a purity of ≥99%. As a small molecule with favorable physicochemical properties, it may have reasonable oral bioavailability, though detailed PK parameters have not been published. Further studies are needed to characterize its absorption, distribution, metabolism, and excretion profile. Standard laboratory practices should be followed for storage and handling.
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| Toxicity/Toxicokinetics |
DMHCA is intended for research use only and is not approved for human therapeutic applications. As a research chemical, comprehensive toxicological data are not available in the publicly accessible literature. Standard safety precautions should be observed when handling this compound, including the use of appropriate personal protective equipment. As with all research chemicals, comprehensive toxicological profiling would be required before any consideration for clinical development. The compound should be handled in well-ventilated areas with proper waste disposal procedures.
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| References | |
| Additional Infomation |
DMHCA (CAS#: 79066-03-8) has a molecular formula of C₂₆H₄₃NO₂ and a molecular weight of 401.63 g/mol. Its IUPAC name is (3β)-3-Hydroxy-N,N-dimethylchol-5-en-24-amide. It is a synthetic oxysterol and a selective LXR agonist. DMHCA induces ABCA1 expression and upregulates FASN and SREBP-1alpha gene expression. It has anti-inflammatory effects and can be used for cholesterol homeostasis and diabetes research. It may serve as a therapeutic agent for atherosclerosis, AMD, and diabetic retinopathy. This compound is not a drug and has not undergone clinical trials.
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| Molecular Formula |
C26H43NO2
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|---|---|
| Molecular Weight |
401.63
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| Exact Mass |
401.329
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| CAS # |
79066-03-8
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| PubChem CID |
24768125
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| Appearance |
White to off-white solid powder
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| LogP |
5.43
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
670
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@H](CCC(=O)N(C)C)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CC=C4[C@@]3(CC[C@@H](C4)O)C)C
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| InChi Key |
NDGUBXOBXSPVHJ-LXVLQKCJSA-N
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| InChi Code |
InChI=1S/C26H43NO2/c1-17(6-11-24(29)27(4)5)21-9-10-22-20-8-7-18-16-19(28)12-14-25(18,2)23(20)13-15-26(21,22)3/h7,17,19-23,28H,6,8-16H2,1-5H3/t17-,19+,20+,21-,22+,23+,25+,26-/m1/s1
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| Chemical Name |
(4R)-4-[(3S,8S,9S,10R,13R,14S,17R)-3-hydroxy-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl]-N,N-dimethylpentanamide
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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: 7.69 mg/mL (19.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.77 mg/mL (1.92 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 7.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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 2: ≥ 0.77 mg/mL (1.92 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 7.7 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 | 2.4899 mL | 12.4493 mL | 24.8985 mL | |
| 5 mM | 0.4980 mL | 2.4899 mL | 4.9797 mL | |
| 10 mM | 0.2490 mL | 1.2449 mL | 2.4899 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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