| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
Glucocorticoid receptor modulator 1 (compound B53), exhibits inhibitory effect on both AP-1 and NF-κB, with IC50 values of 130 nM and 9 nM, respectively [1]. TSLP, MMP-13, TNF-α, CCL-2, IL-6, and IL-1β are among the inflammatory factors whose mRNA expression is decreased by 10 μM of glucose receptor modulator 1 over a 24-hour period [1].
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|---|---|
| ln Vivo |
Glucocorticoid receptor modulator 1 (5, 10 and 20 mg/kg; oral; for 24 days) alleviates dermatitis and reduces the production of inflammatory markers in mice [1].
|
| Cell Assay |
RT-PCR[1]
Cell Types: Mouse macrophage RAW264.7 Tested Concentrations: 10 μM Incubation Duration: 24 hrs (hours) Experimental Results: Actually diminished IL-6, IL-1β, TSLP, MMP-13, TNF-α and CCL-2. Dose-dependently reduces IL-6 and TNF-α with IC50 of 6.90 μM and 7.74 μM, respectively. |
| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse (5 weeks; 2,4-dinitrochlorobenzene-induced atopic dermatitis model) [1]
Doses: 5, 10, and 20 mg/kg Route of Administration: Oral; continuous 24-day Experimental Results: Dramatically improved skin damage and inhibited IL-6, IL-1β, TSLP, and MMP-13 inflammatory factors in a dose-dependent manner. |
| References |
[1]. Li D, Hou T, et al. Discovery and Optimization of N-Acyl-6-sulfonamide-tetrahydroquinoline Derivatives as Novel Non-Steroidal Selective Glucocorticoid Receptor Modulators. J Med Chem. 2022 Nov 18.
|
| Molecular Formula |
C24H23CLN2O4S
|
|---|---|
| Molecular Weight |
470.97
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| CAS # |
2868357-11-1
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| SMILES |
C1(S(NC2C=CC3=C(C=2)CCCN3C(=O)C2=CC=CC=C2)(=O)=O)=CC(Cl)=C(C)C=C1OC
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~212.33 mM)
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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 | 2.1233 mL | 10.6164 mL | 21.2328 mL | |
| 5 mM | 0.4247 mL | 2.1233 mL | 4.2466 mL | |
| 10 mM | 0.2123 mL | 1.0616 mL | 2.1233 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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