Dalcetrapib (JTT-705) - 10mM in DMSO , Cholesteryl ester transfer protein inhibitor, CAS No.211513-37-0, Cholesteryl ester transfer protein inhibitor

CAS: 211513-37-0 Cat. No.: D407978 Fórmula: C₂₃H₃₅NO₂S Peso molecular: 389.59 Número EC: 816-493-8

GRADE & PURITY 10mM in DMSO

Synonyms

RO4607381 | S-2-(1-(2-ethylbutyl)cyclohexanecarboxamido)phenyl 2-methylpropanethioate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Dalcetrapib (JTT-705) Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3.
In vitro

Dalcetrapib modulates CETP activity. Dalcetrapib induces a conformational change in CETP, when added to human plasma. CETP-induced pre-β-HDL formation in human plasma is unchanged by Dalcetrapib ≤3 µM and increased at 10 µM. Dalcetrapib statistically and significantly increases pre-β-HDL formation. Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM. Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner.

In vivo

Treatment with Dalcetrapib leads to significant increases in HDL-C levels. In hamsters injected with [³H]cholesterol-labeled autologous macrophages Dalcetrapib significantly increases fecal elimination of both [³H]neutral sterols and [³H]bile acids. Dalcetrapib increases plasma HDL-[³H]cholesterol. Dalcetrapib has 95% inhibition of CETP activity in male Japanese white rabbits at an oral dose of 30 mg/kg. Dalcetrapib increases the plasma HDL cholesterol level by 27% and 54%, respectively, when given at oral doses of 30 mg/kg or 100 mg/kg once a day for 3 days to male Japanese white rabbits. Treatment with Dalcetrapib markedly increases serum levels of HDL-C. The ratio of HDL2-C to HDL3-C is significantly higher in Dalcetrapib–treated rabbits than in control rabbits at 5 and 7 months, indicating that the inhibition of CETP activity by Dalcetrapib changes the distribution of HDL subfractions and preferentially increases HDL2-C levels. Dalcetrapib treatment increases serum paraoxonase activity and HDL-associated platelet-activating factor acetylhydrolase activity, but decreases the plasma lysophosphatidylcholine concentration.
Cell Data

cell lines：

Concentrations：0-30 μM

Incubation Time：24 hours

Powder Purity:≥97%

Specifications

Sinónimos

RO4607381 | S-2-(1-(2-ethylbutyl)cyclohexanecarboxamido)phenyl 2-methylpropanethioate

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Dalcetrapib (JTT-705) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. Phase 3.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Mecanismo de acción

Cholesteryl ester transfer protein inhibitor

Propiedades del producto

• ALogP: 7.1

Nombres e identificadores

• Isómeros SMILES: CCC(CC)CC1(CCCCC1)C(=O)NC2=CC=CC=C2SC(=O)C(C)C
• RTECS: TZ7260000
• Peso molecular: 389.59
• Reaxy-Rn: 8722148
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8722148&ln=

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro

Preguntas frecuentes

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 211513-37-0, the molecular formula is C23H35NO2S, and the molecular weight is 389.59 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.