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410528-02-8

中文名稱 4-[(1E)-2-[5,6,7,8-四氫-5,5,8,8-四甲基-3-(1H-吡唑-1-基甲基)-2-萘基]乙烯基]苯甲酸
英文名稱 palovarotene
CAS 410528-02-8
分子式 C27H30N2O2
分子量 414.54
MOL 文件 410528-02-8.mol
更新日期 2024/11/30 21:58:08
410528-02-8 結(jié)構(gòu)式 410528-02-8 結(jié)構(gòu)式

基本信息

中文別名
帕羅伐汀
4-[(1E)-2-[5,6,7,8-四氫-5,5,8,8-四甲基-3-(1H-吡唑-1-基甲基)-2-萘基]乙烯基]苯甲酸
英文別名
R 667
Ro 3300074
palovarotene
Unii-28K6I5m16g
R 667
RO 3300074
Palovarotene(R 667)
R667
R 667
R667
RO-3300074
RO 3300074
RO3300074
4-[(E)-2-[5,5,8,8-tetramethyl-3-(pyrazol-1-ylmethyl)-6,7-dihydronaphthalen-2-yl]ethenyl]benzoic acid
(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
所屬類別
生物:小分子化合物

物理化學(xué)性質(zhì)

熔點(diǎn)249-252°C
沸點(diǎn)592.3±50.0 °C(Predicted)
密度1.11
儲存條件Refrigerator
溶解度DMSO(微溶)、乙酸乙酯(微溶、加熱)、甲醇(微溶、加熱)
酸度系數(shù)(pKa)4.26±0.10(Predicted)
形態(tài)固體
顏色白色至灰白色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
Palovarotene 是一種核視網(wǎng)膜酸受體γ (RAR-γ) 激動劑。
靶點(diǎn)

RAR-γ

體內(nèi)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.

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