| Identification | Back Directory | [Name]
PF-06747711 | [CAS]
1892576-58-7 | [Synonyms]
PF-06747711
RORC2 Inverse Agonist
PF06747711,PF 06747711
PF-06747711 >=98% (HPLC)
Benzamide, 3-cyano-N-[1-methyl-3-[1-(2-methyl-1-oxopropyl)-4-piperidinyl]-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl]- | [Molecular Formula]
C26H26F3N5O2 | [MDL Number]
MFCD31697703 | [MOL File]
1892576-58-7.mol | [Molecular Weight]
497.51 |
| Chemical Properties | Back Directory | [Boiling point ]
621.8±55.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 41.67 mg/mL (83.76 mM) | [form ]
Solid | [pka]
10.27±0.43(Predicted) | [color ]
White to off-white | [InChIKey]
BIHPJIJLDNUDGH-UHFFFAOYSA-N | [SMILES]
N#CC1=CC(C(NC2=CN=C(N(C)C=C3C4CCN(C(C(C)C)=O)CC4)C3=C2C(F)(F)F)=O)=CC=C1 |
| Hazard Information | Back Directory | [Uses]
PF-06747711 is a potent, selective, and orally active retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) inverse agonist, with an IC50 of 4.1 nM. Anti-skin inflammatory activity[1]. | [Biological Activity]
PF-06747711 is a mono-imine compound. It regulates gene expression in signaling pathways by targeting a nuclear hormone receptor. It is also used to tre at psoriasis.''PF-06747711 is a potent and selective RORC2 modulator. | [in vivo]
PF-06747711 (10, 30, and 100 mg/kg, p.o., daily over 5 days) inhibits ear swelling in a dose-dependent manner in mice[1]. | Animal Model: | 8?10 week old female Balb/c mice[1] | | Dosage: | 10, 30, and 100 mg/kg | | Administration: | P.O. daily over 5 days | | Result: | Inhibited ear swelling, and caused a maximum inhibition of 46% at 100 mg/kg. |
| [References]
[1] Schnute ME, et al. Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist. J Med Chem. 2018 Sep 9. DOI:10.1021/acs.jmedchem.8b00392 |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|