Chemical Property of Palovarotene
Chemical Property:
- Boiling Point:592.3±50.0 °C(Predicted)
- PKA:4.26±0.10(Predicted)
- PSA:55.12000
- Density:1.11g/cm3
- LogP:6.14900
- Storage Temp.:Refrigerator
- Solubility.:DMSO (Slightly), Ethyl Acetate (Slightly, Heated), Methanol (Slightly, Heated)
- XLogP3:6.8
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:3
- Rotatable Bond Count:5
- Exact Mass:414.230728204
- Heavy Atom Count:31
- Complexity:662
- Purity/Quality:
-
99%, *data from raw suppliers
Palovarotene *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1(CCC(C2=C1C=C(C(=C2)C=CC3=CC=C(C=C3)C(=O)O)CN4C=CC=N4)(C)C)C
- Isomeric SMILES:CC1(CCC(C2=C1C=C(C(=C2)/C=C/C3=CC=C(C=C3)C(=O)O)CN4C=CC=N4)(C)C)C
- Recent ClinicalTrials:A Rollover Study to Further Evaluate the Safety and Efficacy of Palovarotene Capsules in Male and Female Participants Aged ≥14 Years With Fibrodysplasia Ossificans Progressiva (FOP) Who Have Completed the Relevant Parent Studies.
- Recent EU Clinical Trials:A Phase 2, Open-Label, Efficacy and Safety Study of an RARγ-Specific Agonist (Palovarotene) to Prevent Heterotopic Ossification in Subjects with Fibrodysplasia Ossificans Progressiva (FOP)
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Description
Palovarotene an orally bioavailable retinoic acid receptor γ (RARγ) agonist. It increases retinoic acid response element (RARE) activity and decreases NF-κB activity induced by IL-1β in primary mouse stromal cells in reporter assays when used at a concentration of 60 nM. Palovarotene (10 nM) inhibits activin A-induced chondrogenic and osteogenic differentiation of mouse fibro/adipogenic progenitors (FAPs) expressing a mutated form of human activin A receptor type I (ACVR1R206H). It inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1R206H fibrodysplasia ossificans progressiva (FOP) mouse model. Palovarotene (1 mg/kg per day for 14 days) decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury.
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Uses
Palovarotene, is a highly selective retinoic acid receptor gamma (RAR-γ) agonist that is under investigation as a potential treatment for emphysema.