471905-41-6
中文名稱
順式-4-[(4-氯苯基)磺?；鵠-4-(2,5-二氟苯基)環(huán)己烷丙酸
英文名稱
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
CAS
471905-41-6
分子式
C21H21ClF2O4S
分子量
443
MOL 文件
471905-41-6.mol
更新日期
2024/12/23 17:38:45
471905-41-6 結(jié)構(gòu)式
基本信息
中文別名
順式-4-[(4-氯苯基)磺?；鵠-4-(2,5-二氟苯基)環(huán)己烷丙酸順式-4-[(4-氯苯基)磺?；鵠-4-(2,5-二氟苯基)環(huán)己烷丙酸, 一種適度有效的Γ-SECRETASE(Γ-分泌酶)抑制劑
英文別名
CS-10MK-0752/MK0752
MK-0752, >=98%
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid
3-(cis-4-((4-Chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid
Cyclohexanepropanoic acid, 4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-, cis-
3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid
cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid MK-0752
3-((1R,4S)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid, 98%, a moderately potent γ-secretase inhibitor
所屬類別
生物化工：Gamma-secretase 抑制劑物理化學(xué)性質(zhì)
熔點(diǎn)166.6-167.5 °C(Solv: isopropyl acetate (108-21-4); heptane (142-82-5))
沸點(diǎn)616.9±55.0 °C(Predicted)
密度1.361
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度≥22.15 mg/mL in DMSO; insoluble in H2O; ≥48.8 mg/mL in EtOH with ultrasonic
酸度系數(shù)(pKa)4.76±0.10(Predicted)
形態(tài)粉末
顏色White to off-white
常見問題列表
生物活性
MK-0752是一種適度有效的γ-secretase（γ-分泌酶）抑制劑，降低Aβ40產(chǎn)量，IC50為5 nM。Phase 1/2。體外研究
MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation.體內(nèi)研究
MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17. In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain.特征
MK-0752 is a moderately potent γ-secretase inhibitor.靶點(diǎn)
| Target | Value |
| γ secretase(Aβ40) | |
|
Aβ
(in human SH-SY5Y cells) | 5 nM |
體外研究
MK-0752是一種適度有效的γ-分泌抑制劑，其劑量依賴性減少人SH-SY5Y 細(xì)胞中Aβ40，IC50為5 nM。在體外，MK-0752阻斷凹槽胞內(nèi)結(jié)構(gòu)域(ICD)裂解，以及隨后的核易位。
體內(nèi)研究
在獼猴大腦中，MK-0752(240 mg/kg)使新產(chǎn)生的Aβ生成減少，AUV下降90%。此外，MK-0752治療增加Aβ 1-14，Aβ 1-15，和Aβ 1-16水平，而減少Aβ 1-17水平。在豚鼠體內(nèi)，MK-0752 (10 mg/kg -30 mg/kg)口服給藥導(dǎo)致Aβ40在血漿，大腦和腦脊液(CSF)中劑量依賴性減少，在大腦中IC50為440 nM。順式-4-[(4-氯苯基)磺?；鵠-4-(2,5-二氟苯基)環(huán)己烷丙酸價(jià)格(試劑級)
| 報(bào)價(jià)日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
| 2024/11/08 | S2660 | 順式-4-[(4-氯苯基)磺?；鵠-4-(2,5-二氟苯基)環(huán)己烷丙酸 MK-0752 | 471905-41-6 | 5mg | 2213.04元 |
| 2024/11/08 | S2660 | 順式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)環(huán)己烷丙酸 MK-0752 | 471905-41-6 | 10mg | 3011.18元 |
| 2024/11/08 | S2660 | 順式-4-[(4-氯苯基)磺?；鵠-4-(2,5-二氟苯基)環(huán)己烷丙酸 MK-0752 | 471905-41-6 | 10mM(1mL in DMSO) | 3936.04元 |