471905-41-6
中文名称
顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸
英文名称
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
2024/05/27 11:45:58
471905-41-6 结构式
基本信息
中文别名
顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸, 一种适度有效的Γ-SECRETASE(Γ-分泌酶)抑制剂
英文别名
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
所属类别
生物化工：Gamma-secretase 抑制剂物理化学性质
密度1.361
储存条件-20°C储存
溶解度≥22.15 mg/mL in DMSO; insoluble in H2O; ≥48.8 mg/mL in EtOH with ultrasonic
形态粉末
常见问题列表
生物活性
MK-0752是一种适度有效的γ-secretase（γ-分泌酶）抑制剂，降低Aβ40产量，IC50为5 nM。Phase 1/2。体外研究
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.体内研究
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.靶点
| Target | Value |
| γ secretase(Aβ40) | |
|
Aβ
(in human SH-SY5Y cells) | 5 nM |
体外研究
MK-0752是一种适度有效的γ-分泌抑制剂，其剂量依赖性减少人SH-SY5Y 细胞中Aβ40，IC50为5 nM。在体外，MK-0752阻断凹槽胞内结构域(ICD)裂解，以及随后的核易位。
体内研究
在猕猴大脑中，MK-0752(240 mg/kg)使新产生的Aβ生成减少，AUV下降90%。此外，MK-0752治疗增加Aβ 1-14，Aβ 1-15，和Aβ 1-16水平，而减少Aβ 1-17水平。在豚鼠体内，MK-0752 (10 mg/kg -30 mg/kg)口服给药导致Aβ40在血浆，大脑和脑脊液(CSF)中剂量依赖性减少，在大脑中IC50为440 nM。顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | S2660 | 顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸 MK-0752 | 471905-41-6 | 5mg | 2213.04元 |
| 2024/04/30 | S2660 | 顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸 MK-0752 | 471905-41-6 | 10mM(1mL in DMSO) | 3936.04元 |
| 2024/04/30 | S2660 | 顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸 MK-0752 | 471905-41-6 | 50mg | 7923.68元 |