顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸
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 |
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中文同义词 | 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;3-(顺式-4-((4-氯苯基)磺酰基)-4-(2,5-二氟苯基)环己基)丙酸;MK-0752,Γ-SECRETASE(Γ-分泌酶)抑制剂 |
英文名称 | cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid |
英文同义词 | MK-0752, >=98%;Cyclohexanepropanoic acid, 4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)-, cis-;MK-0752/MK0752;3-(cis-4-((4-Chlorophenyl)sulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid;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;cis-4-[(4-Chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexanepropanoic acid;CS-10 |
CAS号 | 471905-41-6 |
分子式 | C21H21ClF2O4S |
分子量 | 442.9 |
EINECS号 | |
相关类别 | 小分子抑制剂,天然产物;小分子抑制剂;信号转导通路激酶抑制剂;蛋白酶;Inhibitor;Inhibitors |
Mol文件 | 471905-41-6.mol |
结构式 |
顺式-4-[(4-氯苯基)磺酰基]-4-(2,5-二氟苯基)环己烷丙酸 性质
熔点 | 166.6-167.5 °C(Solv: isopropyl acetate (108-21-4); heptane (142-82-5)) |
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沸点 | 616.9±55.0 °C(Predicted) |
密度 | 1.361 |
储存条件 | Store at -20°C |
溶解度 | DMSO 中≥22.15 mg/mL;不溶于水; ≥48.8 mg/mL,乙醇溶液,超声波 |
形态 | 粉末 |
酸度系数(pKa) | 4.76±0.10(Predicted) |
颜色 | 白色至米白色 |
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。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.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.MK-0752 is a moderately potent γ-secretase inhibitor.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。
Target | Value |
γ secretase(Aβ40) | |
Aβ
(in human SH-SY5Y cells) | 5 nM |
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。
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。安全信息
海关编码 | 29163990 |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | 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 |
2024/08/19 | 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 | 10mg | 3011.18元 |