2413986-35-1
2413986-35-1 structure
- Name: RORγt Inverse agonist 10
- Chemical Name: RORγt Inverse agonist 10
- CAS Number: 2413986-35-1
- Molecular Formula: C25H26F6N6O3
- Molecular Weight: 572.50
- Catalog: Signaling Pathways Metabolic Enzyme/Protease ROR
- Create Date: 2020-08-09 13:10:46
- Modify Date: 2024-01-04 20:40:12
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RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R[1]
| Name | RORγt Inverse agonist 10 |
|---|
| Description | RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R[1] |
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| Related Catalog | |
| Target |
RORγt:51 nM (IC50) |
| In Vitro | RORγt Inverse agonist 10 has a good liver microsome stability (human CLint=0.010 mL/min/mg, mouse CLint=0.030 mL/min/mg)[1]. RORγt Inverse agonist 10 suppresses the IL-17A production in a dose-dependent manner with an IC50 of 130 nM in a human whole-blood assay[1]. |
| In Vivo | RORγt Inverse agonist 10 (3-100 mg/kg; p.o.) shows robust and dose-dependent inhibitory effect on the IL-17A production in mouse IL-18/23-induced cytokine expression model[1]. RORγt Inverse agonist 10 (1.145 mg/kg; p.o.) shows a high AUC of 15000 nM*h and t1/2 of 3.6 hours[1]. Animal Model: C57/BL6 male mice, mouse IL-18/23-induced cytokine expression model[1] Dosage: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration Result: Significantly inhibited the IL-17A production in a dose-dependent manner. Animal Model: Mice[1] Dosage: 1.145 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: AUC=15000 nM*h, t1/2=3.6 hours. |
| References |
| Molecular Formula | C25H26F6N6O3 |
|---|---|
| Molecular Weight | 572.50 |