中文名 | Palovarotene |
英文名 | Palovarotene |
别名 | 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 |
英文别名 | R 667 Ro 3300074 RO 3300074 Palovarotene palovarotene Unii-28K6I5m16g Palovarotene(R 667) (E)-4-(2-(3-((1H-pyrazol-1-yl)Methyl)-5,5,8,8-tetraMethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid 4-[(1E)-2-[5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-3-(1H-pyrazol-1-ylmethyl)-2-naphthalenyl]ethenyl]benzoic acid |
CAS | 410528-02-8 |
EINECS | 200-258-5 |
化学式 | C27H30N2O2 |
分子量 | 414.54 |
密度 | 1.11 |
熔点 | 249-252°C |
沸点 | 592.3±50.0 °C(Predicted) |
溶解度 | DMSO (微溶),乙酸乙酯 (微溶,加热),甲醇 (微溶,加热) |
酸度系数 | 4.26±0.10(Predicted) |
存储条件 | Refrigerator |
外观 | 固体 |
颜色 | White to Off-White |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.412 ml | 12.062 ml | 24.123 ml |
5 mM | 0.482 ml | 2.412 ml | 4.825 ml |
10 mM | 0.241 ml | 1.206 ml | 2.412 ml |
5 mM | 0.048 ml | 0.241 ml | 0.482 ml |
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