RORγt inverse agonist 34
RORγt inverse agonist 34 (compound 5a) is a RORγt inverse agonist with an IC50 of 0.094 μM for RORγt-LBD. RORγt inverse agonist 34 is used for psoriasis research.
For research use only. We do not sell to patients.
- CAS No.: 2247604-77-7
- Formula: C31H37N3O3S
- Molecular Weight:531.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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RORγt 0.094 μM (IC50) |
RORγt inverse agonist 34 (2h) impacts the recruitment of SRC1 coactivating peptide by RORγt-LBD with an IC50 of 0.094 μM[1].
RORγt inverse agonist 34 inhibits the differentiation of Th17 cells effectively with an IC50 of 1.57 μM[1].
RORγt inverse agonist 34 (1 μM, 1 h) exhibits a half-life of 18 min in mouse liver microsomes [1].
RORγt inverse agonist 34 (2.5 min) inhibits hERG with the IC50 of surpassed 40 μM, showing low toxicity to heart[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RORγt inverse agonist 34 (0.25%-4% ointment, daily, 11 days) exhibits anti-psoriasis effects in Imiquimod (HY-B0180) induced psoriatic mice model[1].
RORγt inverse agonist 34 (4% ointment, transdermal administration, applied to the skin with a force of approximately 50 g ) in plasma reaches its peak at approximately 10 min with 0.075 μg/mL in BALB/c mice [1].
RORγt inverse agonist 34 (10%-20% ointment, daily, 12days) has no significant acute toxicity in BALB/c mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The Imiquimod (HY-B0180) -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 (HY-B0180) from day 1 to day 7. The mice in the normal group had a Vaseline Lanette cream applied as an alternative treatment[1].
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Dosage:100 mg/kg
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Administration:i.p.,daily 7days
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Result: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 (HY-B0180B) -induced abnormal spleen enlargement, which is comparable to the positive control Dexamethasone (HY-14648) 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 (HY-14648) (5 mg/kg).
Inhibited the erythema and scaling for the back skinwas essentially comparable to that of Dexamethasone (HY-14648).
Chemical Information
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CAS No. 2247604-77-7
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Molecular Weight 531.71
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Formula C31H37N3O3S
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SMILES
O=S(N1CCCC2=CC(NC3=CC4=C(C=C3)C(CCC4)=O)=CC=C21)(N(CC5=CC=C(C=C5)C(C)(C)C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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