| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
RORγt 120 nM (Ki)
7β,27-Dihydroxycholesterol targets the retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. As an agonist, it activates RORγ- or RORγt-dependent signaling. It promotes the differentiation of mouse and human CD4⁺ Th17 cells. The compound is a potent and selective activator of RORγt with a Kᵢ of 120 nM. It functions as a bioactive lipid involved in cholesterol homeostasis and cellular signaling. |
|---|---|
| ln Vitro |
In vitro treatments of 7ß,27-Dihydroxycholesterol (0.3 μM or 6 μM; 2 h) stimulate the production of IL-17 in human and mouse Th17 cells [1].
In vitro, 7β,27-Dihydroxycholesterol activates RORγ- or RORγt-dependent signaling with EC₅₀ values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. It promotes the differentiation of mouse and human CD4⁺ Th17 cells. The compound is a potent and selective RORγt agonist with a Kᵢ of 120 nM. These activities make it useful for studying oxysterol signaling and Th17 cell biology. |
| ln Vivo |
In mice, 7ß,27-Dihydroxycholesterol (60 mg/kg; subcutaneous injection; twice daily for 3 days) increases the production of IL-17 [1].
In vivo, 7β,27-Dihydroxycholesterol is used in biomedical research to study lipid metabolism, nuclear receptor regulation, and inflammatory responses. Its role as an oxysterol agonist of RORγt suggests potential effects on Th17-driven inflammatory responses in vivo. The compound is also studied for its involvement in cardiovascular, metabolic, and neurodegenerative disease mechanisms. Specific in vivo efficacy data are not detailed in the available sources. |
| Enzyme Assay |
Non-cell-based enzyme/receptor binding assays for 7β,27-Dihydroxycholesterol typically involve competitive binding studies using purified RORγ or RORγt protein. Standard protocols include incubating varying concentrations of the test compound with the receptor ligand-binding domain and a radiolabeled or fluorescent probe in appropriate buffer systems, followed by separation of bound from free ligand via filtration or fluorescence polarization. Binding affinity (Kᵢ values) is calculated using nonlinear regression analysis. The compound shows a Kᵢ of 120 nM for RORγt. Surface plasmon resonance (SPR) may also be employed.
|
| Cell Assay |
Cell-based assays for 7β,27-Dihydroxycholesterol typically utilize reporter gene assays with HEK293T cells expressing recombinant human RORγ or RORγt and a luciferase reporter. Standard protocols involve culturing cells in appropriate media at 37°C in 5% CO₂, followed by treatment with varying concentrations of the compound (typically 0.01-100 μM) for 18-24 hours. Reporter gene activity is quantified by luminescence. EC₅₀ values are calculated from dose-response curves. The compound shows EC₅₀ of 691 nM for RORγ and 1,045 nM for RORγt. Th17 cell differentiation assays are also used.
|
| Animal Protocol |
In vivo animal studies for 7β,27-Dihydroxycholesterol typically involve administration in rodent models to study lipid metabolism, inflammatory responses, or disease mechanisms. Standard protocols include dosing at ranges of 1-50 mg/kg body weight via oral gavage, intraperitoneal injection, or intravenous injection, with observations over 7-14 days depending on the study objectives. Pharmacodynamic assessments may include blood sampling for oxysterol analysis, tissue collection for histopathological examination, and monitoring of body weight and general health parameters. All animal studies must comply with institutional ethical guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for 7β,27-Dihydroxycholesterol are consistent with an oxysterol. The compound has a molecular weight of 418.65 g/mol and shows solubility in DMF (2 mg/mL), ethanol (20 mg/mL), and ethanol:PBS (1:2) (0.30 mg/mL). It should be stored as a crystalline solid at -20°C. For in vivo administration, formulations using suitable vehicles may be employed. Definitive PK parameters such as half-life, Cmax, and AUC require formal studies. The compound is generated through enzymatic and oxidative processes.
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| References | |
| Additional Infomation |
7β,27-Dihydroxycholesterol is a bile acid.
7β,27-Dihydroxycholesterol is a dihydroxylated oxysterol derived from cholesterol metabolism and an agonist of RORγ and RORγt. It promotes the differentiation of Th17 cells and is used in biomedical research to study lipid metabolism, nuclear receptor regulation, and inflammatory responses. The compound is also studied for its role in cardiovascular, metabolic, and neurodegenerative disease mechanisms. It is not an approved drug and has not undergone clinical trials; it is strictly for research purposes. |
| Molecular Formula |
C27H46O3
|
|---|---|
| Molecular Weight |
418.65
|
| Exact Mass |
418.345
|
| CAS # |
240129-43-5
|
| PubChem CID |
52931518
|
| Appearance |
White to off-white solid powder
|
| LogP |
5.331
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
30
|
| Complexity |
644
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C[C@H](CCC[C@@H](C)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2[C@H](C=C4[C@@]3(CC[C@@H](C4)O)C)O)C)CO
|
| InChi Key |
RXMHNAKZMGJANZ-BMOLSTJGSA-N
|
| InChi Code |
InChI=1S/C27H46O3/c1-17(16-28)6-5-7-18(2)21-8-9-22-25-23(11-13-27(21,22)4)26(3)12-10-20(29)14-19(26)15-24(25)30/h15,17-18,20-25,28-30H,5-14,16H2,1-4H3/t17-,18-,20+,21-,22+,23+,24+,25+,26+,27-/m1/s1
|
| Chemical Name |
(3S,7R,8S,9S,10R,13R,14S,17R)-17-[(2R,6R)-7-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthrene-3,7-diol
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.3886 mL | 11.9432 mL | 23.8863 mL | |
| 5 mM | 0.4777 mL | 2.3886 mL | 4.7773 mL | |
| 10 mM | 0.2389 mL | 1.1943 mL | 2.3886 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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