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Palovarotene(R 667)

CAS number:410528-02-8    molecular formula:C27H30N2O2

overview

compound introduction

Palovarotene is a nuclear retinoic acid receptor γ ( RAR-γ ) agonist. In Vivo Palovarotene suppresses post-traumatic chondrogenesis and osteogenesis and mitigated trauma-induced ectopic bone formation. Palovarotene inhibits subcutaneous and intramuscular heterotopic ossification (HO) in mice. Palovarotene is given orally for 14 days at 1 mg/kg/day starting on post-operative day (POD) 1 or POD-5, and HO amount, wound dehiscence and related processes are monitored for up to 84 days post injury. Compared to vehicle-control animals, Palovarotene significantly decreases HO by 50 to 60% regardless of when the treatment started and if infection is present . Starting from day 1 of injury, half of the Acvr1 cR206H/+ mice are treated with Palovarotene by daily gavage for 14 days and the other half received vehicle as control. Analysis by mCT and 3D image reconstruction at day 14 shows that large HO tissue masses have formed in the targeted leg of Acvr1 cR206H/+ mutant mice receiving vehicle, but HO formation is greatly diminished in Palovarotene-treated companions by more than 80% based on bone volume/total volume quantification. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:RAR-γ

Specs

Chinese alias帕洛瓦罗泰内 | 帕罗伐汀 | 4-[(1E)-2-[5,6,7,8-四氢-5,5,8,8-四甲基-3-(1H-吡唑-1-基甲基)-2-萘基]乙烯基]苯甲酸
English aliasPALOVAROTENE [INN] | Ro 3300074 | A914214 | DB12320 | Palovarotene [USAN] | GTPL8276 | 4-((1E)-2-(5,5,8,8-Tetramethyl-3-(1H-pyrazol-1-ylmethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)ethenyl)benzoic acid | Palovarotene [USAN:INN] | 4-((1E)-2-(5,5,8,8-Tetrameth
CAS number410528-02-8molecular formulaC27H30N2O2
molecular weight414.54 g/molExact mass≥99%
PSA55.100 Ųlogp6.8

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