Palovarotene

Palovarotene an orally bioavailable retinoic acid receptor gamma (RARgamma) agonist. It increases retinoic acid response element (RARE) activity and decreases NF-kappaB activity induced by IL-1beta 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.Formal Name: 4-[(1E)-2-[5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-3-(1H-pyrazol-1-ylmethyl)-2-naphthalenyl]ethenyl]-benzoic acid. CAS Number: 410528-02-8. Synonyms: Ro 3300074. Molecular Formula: C27H30N2O2. Formula Weight: 414.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 25 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.3 mg/ml, Ethanol: 3 mg/ml. lambdamax: 321 nm. SMILES: CC1(C)CCC(C)(C)C2=C1C=C(CN3C=CC=N3)C(/C=C/C4=CC=C(C(O)=O)C=C4)=C2. InChi Code: InChI=1S/C27H30N2O2/c1-26(2)12-13-27(3,4)24-17-22(18-29-15-5-14-28-29)21(16-23(24)26)11-8-19-6-9-20(10-7-19)25(30)31/h5-11,14-17H,12-13,18H2,1-4H3,(H,30,31)/b11-8+. InChi Key: YTFHCXIPDIHOIA-DHZHZOJOSA-N.