| Targets |
RORγt 0.094 μM (IC50)
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|---|---|
| ln Vitro |
RORγt inverse agonist 34 affects the recruitment of SRC1 coactivator peptide by RORγt-LBD with an IC50 of 0.094 μM[1]. RORγt inverse agonist 34 effectively inhibits Th17 cell differentiation with an IC50 of 1.57 μM[1]. The half-life of RORγt inverse agonist 34 (1 μM, 1 h) in mouse liver microsomes is 18 min[1]. RORγt inverse agonist 34 inhibits hERG with an IC50 of more than 40 μM, indicating low cardiotoxicity[1].
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| ln Vivo |
RORγt inverse agonist 34 (100 mg/kg, ip, daily, 7 days) showed significant effect in improving Imiquimod-induced psoriasis lesions[1]. RORγt inverse agonist 34 (0.25% - 4% ointment, daily, 11 days) showed anti-psoriatic effects in the Imiquimod-induced psoriasis mouse model [1]. In BALB/c mice, RORγt inverse agonist 34 (4% ointment, transdermal administration, dosage approximately 50 g) reaches a peak plasma concentration of 0.075 μg/mL in approximately 10 minutes [1]. RORγt inverse agonist 34 (10% - 20% mg/kg ointment, daily, 12 days) showed no significant acute toxicity in BALB/c mice [1].
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| Animal Protocol |
Animal/Disease Models: The Imiquimod -induced psoriasis model was established with female BALB/c mice aged 8 to 10 weeks. A 2 cm × 3 cm area of hair on the backs of the mice was shaved using a depilatory cream to establish experimental areas. The shaved backs and right ears of the mice were treated with a daily topical dose of 62.5 mg of a commercially available 5% Imiquimod from day 1 to day 7. The mice in the normal group had a Vaseline Lanette cream applied as an alternative treatment[1].
Doses: 100 mg/kg Route of Administration: i.p.,daily 7days Experimental Results: Demonstrated notable anti-inflammatory properties in the mouse model of psoriasis, with the most prominent effects observed at a dose of 4%. Demonstrated significant efficacy in mitigating the Lmiquimod -induced abnormal spleen enlargement, which is comparable to the positive control Dexamethasone by comparing the ratios of splenic weight to body weight among different groups of mice. Exhibited more significant effects in alleviating ear inflammation compared to the positive control Dexamethasone (5 mg/kg). Inhibited the erythema and scaling for the back skinwas essentially comparable to that of Dexamethasone. |
| References |
| CAS # |
2247604-77-7
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|---|---|
| Appearance |
Typically exists as solids at room temperature
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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)
|
| 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.) |
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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