| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
pEC50: 6.6 (LRH-1) and 7.5 (SF-1)[1]
RJW100 targets two nuclear receptors: liver receptor homolog 1 (LRH-1/NR5A2) and steroidogenic factor-1 (SF-1/NR5A1). It acts as an agonist at both receptors, modulating transcriptional activity involved in metabolic regulation, steroid hormone production, and reproductive function. |
|---|---|
| ln Vitro |
Treatment with RJW100 (compound 24-exo) causes a notable increase in small/short heterodimer partner (SHP) transcripts at 5 µM, which is dose-dependent[1]. The bound PIP2 phospholipid from SF-1 is almost entirely displaced by RJW100 (compound 24-exo) at 1 µM[1]. A distinct dose-dependent shift in the native PAGE movement of hLRH-1 LBD (ligand binding domain) post RJW100 (compound 24-exo; 0-100 µM) binding is seen when hLRH-1 LBD is used alone, without any phospholipid complexation[1]. ZEB1 and ZEB2 protein downregulation is both strongly induced by RJW100 and strongly activates the miR-200c promoter[2].
In vitro, RJW100 exhibits potent agonist activity on LRH-1 with a pEC50 of 6.6, and on SF-1 with a pEC50 of 7.5. It effectively activates the miR-200c promoter at 5 uM, with dose-dependent increases in small heterodimer partner (SHP) transcript levels. |
| Enzyme Assay |
A standard radioligand binding assay can be performed by incubating purified LRH-1 or SF-1 receptor proteins with varying concentrations of RJW100 (0.1 nM-10 uM) in binding buffer for 2-4 h at 4degC, followed by separation of bound and free ligand using charcoal-dextran or filtration methods, then scintillation counting to measure binding affinity.
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| Cell Assay |
RT-PCR[1]
Cell Types: HEK293 cells Tested Concentrations: 1 µM, 5 µM, 10 µM Incubation Duration: 24 hrs (hours) Experimental Results: Induced a significant dose-dependent increase in SHP transcripts beginning at 5 µM. For cellular activation assays, cells expressing LRH-1 or SF-1 are seeded in 96-well plates and treated with RJW100 (0.01-10 uM) for 24 h. Luciferase reporter activity is measured, or qPCR is performed to assess downstream target gene expression such as SHP or miR-200c. EC50 values are determined by nonlinear regression. |
| Animal Protocol |
A typical in vivo study involves administering RJW100 (0.1-5 mg/kg) to mice via oral gavage or intraperitoneal injection. After a predetermined period, tissues are collected for qPCR or Western blot analysis of LRH-1/SF-1 target genes, with plasma samples collected for pharmacokinetic evaluation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for RJW100 are limited. As a small-molecule nuclear receptor agonist, it is expected to have moderate oral bioavailability and plasma exposure following oral administration. Typical PK parameters such as half-life (t1/2), Cmax, and AUC would be determined in rodent models by standard LC-MS/MS analysis of plasma samples collected over 24 h post-dose.
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| Toxicity/Toxicokinetics |
Toxicological studies have not been extensively reported for RJW100. As a research tool compound not intended for human use, standard safety assessments may include general observation in rodent models, body weight monitoring, and histopathological evaluation of major organs at the conclusion of in vivo experiments.
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| References |
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| Additional Infomation |
RJW100 is classified as a potent and selective agonist for LRH-1 and SF-1, and is used as a valuable chemical probe to study the biological functions of these nuclear receptors. It has not yet entered human clinical trials and remains an investigational research compound exclusively used in preclinical settings.
|
| Molecular Formula |
C28H34O
|
|---|---|
| Molecular Weight |
386.57
|
| Exact Mass |
386.261
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| CAS # |
1276664-20-0
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| PubChem CID |
52936713
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| Appearance |
Colorless to light yellow ointment
|
| LogP |
7.285
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
1
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
29
|
| Complexity |
589
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
[C@H]1(O)[C@@]2([H])[C@](C(C3=CC=CC=C3)=C)(C(C3=CC=CC=C3)=C(CCCCCC)C2)CC1
|
| InChi Key |
ZFXMYHPLTQTTFW-REUBFRLUSA-N
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| InChi Code |
InChI=1S/C28H34O/c1-3-4-5-8-17-24-20-25-26(29)18-19-28(25,21(2)22-13-9-6-10-14-22)27(24)23-15-11-7-12-16-23/h6-7,9-16,25-26,29H,2-5,8,17-20H2,1H3/t25-,26+,28-/m0/s1
|
| Chemical Name |
(1R,3aR,6aR)-5-hexyl-4-phenyl-3a-(1-phenylethenyl)-2,3,6,6a-tetrahydro-1H-pentalen-1-ol
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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) |
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
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|---|---|
| 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 | 2.5869 mL | 12.9343 mL | 25.8685 mL | |
| 5 mM | 0.5174 mL | 2.5869 mL | 5.1737 mL | |
| 10 mM | 0.2587 mL | 1.2934 mL | 2.5869 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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