JTE-151
Based on 1 Customer Validation
JTE-151 is an orally active, selective RORγ antagonist with IC50 values of 20.6 nM, 41.8 nM and 32.2 nM against hRORγ, rRORγ and mRORγ, respectively. JTE-151 reduces the production of IL-17. JTE-151 alleviates paw swelling and bone destruction in arthritis models. JTE-151 can be used in research related to rheumatoid arthritis, collagen-induced arthritis, experimental autoimmune encephalomyelitis, psoriasis, multiple sclerosis and inflammatory bowel disease.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.34%
- CAS. Nr.: 1404380-58-0
- Formel: C28H37ClN2O4
- Molecular Weight:501.06
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
|
hRORγ 20.6 nM (IC50) |
rRORγ 41.8 nM (IC50) |
mRORγ 32.2 nM (IC50) |
IL-17 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
2.3 μM
Compound: 53
|
Agonist activity at human RoRc-LBD expressed in CHO cells assessed as transcriptional activity by GAL4 reporter assay
Agonist activity at human RoRc-LBD expressed in CHO cells assessed as transcriptional activity by GAL4 reporter assay
|
[PMID: 24502334] |
JTE-151 (0.0001-1 nM) potently and selectively inhibits the transcriptional activity of hRORγ, rat RORγ, and mouse RORγ, with IC50 values of 20.6 nM, 41.8 nM, and 32.2 nM, respectively, and exhibits extremely low activity against other nuclear receptors[2].
JTE-151 exhibits highly selective inhibitory activity against RORγ, with extremely low activity against most off-target nuclear receptors, receptors, enzymes, and cytochrome P450 subtypes[3].
JTE-151 shows no mutagenic activity in the bacterial reverse mutation assay using 5 strains[3].
JTE-151 does not induce chromosomal aberrations in cultured CHL mammalian cells[3].
JTE-151 (0.0001-10 μM; 72 h) selectively inhibits the differentiation of naive mouse CD4+ T cells into Th17 cells, with an IC50 of 32.4 nM. At concentrations of 0.3 μmol/L and higher, it reduces the expression of Th17-related genes (Il17a, Il17f, Il22, Il23r), without affecting the differentiation of cells into Th1, Th2 or Treg cells, nor does it affect the expression of the Rorc gene[2].
JTE-151 (0.0001-1 μM; 72 h) specifically inhibits IL-17 production by activated helper T cells, with an IC50 of 27.7 nM, and does not affect the production of IFN-γ or IL-4[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
JTE-151 (3-30 mg/kg; p.o.; once daily; for consecutive 21 days) inhibits inflammatory responses and reduction of bone mineral density in rats with adjuvant-induced arthritis[1].
JTE-151 (1-30 mg/kg; p.o.; once daily; for 8 days) dose-dependently inhibits antigen-induced IL-17 production in female C57BL/6J mice, with significant inhibition observed at doses of 1 mg/kg and higher[2].
JTE-151 (3-30 mg/kg; p.o.; daily; days 22 to 36) ameliorates collagen-induced arthritis in male DBA/1J mice, and doses of 3 mg/kg and higher significantly reduce arthritis severity when administered from days 22 to 36[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:LEW/CrlCrlj (female, 6-week-old, collagen-induced arthritis model)[1]
-
Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg (prophylactic); 30 mg/kg (therapeutic)
-
Administration:p.o.; daily; 21 days (prophylactic); p.o.; daily; 14 days (therapeutic)
-
Result:Significantly suppressed hindpaw swelling on day 22 at 1 mg/kg or higher.
Significantly reduced inflammatory cell infiltration and synovial cell hyperplasia scores at 3 mg/kg or higher.
Significantly inhibited tarsal bone density loss and reduced μCT-detected bone destruction at 1 mg/kg or higher.
Significantly suppressed synovial mRNA levels of Th17-related genes (IL-17A, RORC, CCR6, IL-23R) at all prophylactic doses.
Partially but significantly decreased hindpaw swelling on day 29 with 30 mg/kg therapeutic dose.
Significantly suppressed synovial IL-17A, RANKL, and MMP-3 mRNA levels and increased tarsal bone density compared to vehicle with 30 mg/kg therapeutic dose.
Tended to reduce RORC mRNA levels with 30 mg/kg therapeutic dose.
-
Animal Model:LEW/CrlCrlj (male, 6-week-old, adjuvant-induced arthritis model)[1]
-
Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg (prophylactic); 30 mg/kg (therapeutic)
-
Administration:p.o.; daily; 21 days (prophylactic); p.o.; daily; 14 days (therapeutic)
-
Result:Significantly suppressed hindpaw swelling and tarsal bone density loss on day 22 at 3 mg/kg or higher prophylactic dose.
Significantly suppressed hindpaw swelling and tarsal bone density loss on day 29 with 30 mg/kg therapeutic dose.
-
Animal Model:C57BL/6J (female, 7-week-old, experimental autoimmune encephalomyelitis model)[2]
-
Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
-
Administration:p.o.; daily; 8 days
-
Result:Significantly inhibited the increase in plasma IL-17 concentration at all tested doses.
Dose-dependently reduced plasma IL-17 levels, with the lowest levels observed at 30 mg/kg.
-
Animal Model:DBA/1J (male, 6-week-old, collagen-induced rheumatoid arthritis model)[2]
-
Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
-
Administration:p.o.; daily; 15 days (day 22 to day 36)
-
Result:Significantly reduced mean arthritis scores at doses of 3 mg/kg and higher compared to the vehicle group on day 36.
Showed the greatest reduction in arthritis severity at 30 mg/kg, with a statistically significant lower mean score than the vehicle group.
Chemical Information
-
CAS. Nr. 1404380-58-0
-
Appearance Solid
-
Molecular Weight 501.06
-
Formel C28H37ClN2O4
-
Color Off-white to light yellow
-
SMILES
ClC1=CC(C)=CC=C1NC(C[C@H](CCC(O)=O)C2=NOC([C@@H]3C[C@H](CC(C)(C)C)C3)=C2C4CC4)=O
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (49.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
-
Data Sheet (280 KB)
-
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Arita K, et al. Suppressive Effects of JTE-151, a Novel Orally Available RORγ Antagonist, in Experimental Models of Rheumatoid Arthritis. Biological & pharmaceutical bulletin. 2025;48(7):1118-1124. [Content Brief]
[2]. Arita K, et al. Pharmacological Properties of JTE-151; A Novel Orally Available RORγ Antagonist That Suppresses Th17 Cell-Related Responses in Vitro and in Vivo. Biol Pharm Bull. 2024;47(12):2050-2057. [Content Brief]
[3]. Maeba T, et al. Discovery and SAR of JTE-151: A Novel RORγ Inhibitor for Clinical Development. Journal of medicinal chemistry. 2024 Jan 25;67(2):952-970. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9958 mL | 9.9788 mL | 19.9577 mL | 49.8942 mL |
| 5 mM | 0.3992 mL | 1.9958 mL | 3.9915 mL | 9.9788 mL | |
| 10 mM | 0.1996 mL | 0.9979 mL | 1.9958 mL | 4.9894 mL | |
| 15 mM | 0.1331 mL | 0.6653 mL | 1.3305 mL | 3.3263 mL | |
| 20 mM | 0.0998 mL | 0.4989 mL | 0.9979 mL | 2.4947 mL | |
| 25 mM | 0.0798 mL | 0.3992 mL | 0.7983 mL | 1.9958 mL | |
| 30 mM | 0.0665 mL | 0.3326 mL | 0.6653 mL | 1.6631 mL | |
| 40 mM | 0.0499 mL | 0.2495 mL | 0.4989 mL | 1.2474 mL |
JTE-151 Related Classifications
HY-155487 Related Classifications
Powered by Bioz