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261947-38-0

中文名稱 CP 532623
CAS 261947-38-0
分子式 C27H27F9N2O3
分子量 598.5
MOL 文件 261947-38-0.mol
261947-38-0 結(jié)構(gòu)式 261947-38-0 結(jié)構(gòu)式

基本信息

英文別名
CP 532623
CP 532623 >=98% (HPLC)
(2R,4S)-4-[Acetyl[[3,5-bis(trifluoromethyl)phenyl]methyl]amino]-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-1(2H)-quinolinecarboxylic acid 1-methylethyl ester
1(2H)-Quinolinecarboxylic acid, 4-[acetyl[[3,5-bis(trifluoromethyl)phenyl]methyl]amino]-2-ethyl-3,4-dihydro-6-(trifluoromethyl)-, 1-methylethyl ester, (2R,4S)-

物理化學(xué)性質(zhì)

儲存條件2-8°C
溶解度在DMSO中的溶解度為20mg/mL,澄清
形態(tài)粉末
顏色白色至米色

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
WGK Germany3

常見問題列表

生物活性
CP-532623 是 CETP 抑制劑,可提高高密度脂蛋白膽固醇水平。CP-532623 與 Torcetrapib 的結(jié)構(gòu)相似,并具有高度親脂性。
靶點

CETP

體外研究

CP-532623 is highly lymphatically transported (28% of dose), and lymphatic transport is closely correlated with drug affinity for ex-vivo lymph lipoproteins or triglyceride emulsions and poorly relates to solubility in mixtures of lipoprotein core and/or surface lipids. CP-532623 alters the kinetics of lymph lipid transport and decreases lymph lipid transport in chylomicrons.

體內(nèi)研究

CP-532623 (50 mg; oral administration; adult male greyhound dogs) treatment substantially transports into the lymphatic system (>25% dose) in fed and fasted dogs. Food enhances oral bioavailability (from 44 to 58%, respectively) and the proportion of the absorbed dose transports via the lymph (from 61 to 86% and from 68 to 83%, respectively). Lymphatic triglyceride transport is significantly lower in fed dogs administered CP-532623.

Animal Model: Adult male greyhound dogs (27-39 kg)
Dosage: 50 mg
Administration: Oral administration with a long-chain lipid formulation to fed lymphcannulated
Result: Substantially transported into the lymphatic system (>25% dose) in fed and fasted dogs. Food enhanced oral bioavailability and the proportion of the absorbed dose transported via the lymph.
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