MK-0752 - Moligand™, 10mM in DMSO , CAS No.471905-41-6

CAS: 471905-41-6 Cat. No.: M408821 分子式: C₂₁H₂₁ClF₂O₄S 分子量: 442.91 EC番号: 684-251-7

グレード＆純度 Moligand™, 10mM in DMSO

Synonyms

3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

MK-0752 is a moderately potentγ-secretaseinhibitor, which reduces Aβ40 production withIC50of 5 nM. Phase 1/2.
In vitro

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.

In vivo

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.
Cell Data

cell lines：HNSCC cell line, UM-SCC-17B

Concentrations：

Incubation Time：

Powder Purity:≥99%

仕様

同義語

3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

名前と識別子

異性体SMILES

C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl

分子量

442.91

Reaxy-Rn

25469521

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25469521&ln=

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro DMSO: 27 mg/mL (198.31 mM); Ethanol: 27 mg/mL (198.31 mM); Water: Insoluble