1. Metabolic Enzyme/Protease
  2. CETP
  3. Dalcetrapib

Dalcetrapib (Synonyms: JTT-705; RO4607381)

Cat. No.: HY-14950 Purity: 99.46%
Handling Instructions

Dalcetrapib (JTT-705; RO-4607381) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol.

For research use only. We do not sell to patients.

Dalcetrapib Chemical Structure

Dalcetrapib Chemical Structure

CAS No. : 211513-37-0

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10 mM * 1 mL in DMSO USD 218 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 358 In-stock
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50 mg USD 948 In-stock
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100 mg USD 1320 In-stock
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Description

Dalcetrapib (JTT-705; RO-4607381) is a rhCETP inhibitor with IC50 of 0.2 μM that increases the plasma HDL cholesterol. IC50 value: 0.2 uM [1] Target: CETP 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 [1]. Dalcetrapib achieves 50% inhibition of CETP activity in human plasma at a concentration of 9 μM [2]. Dalcetrapib inhibits the CETP activity of media in HepG2 in a dose-dependent manner [3]. 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 [1]. 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 [2].

Clinical Trial
Molecular Weight

389.59

Formula

C₂₃H₃₅NO₂S

CAS No.

211513-37-0

SMILES

CC(C)C(SC1=C(NC(C2(CC(CC)CC)CCCCC2)=O)C=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (128.34 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5668 mL 12.8340 mL 25.6680 mL
5 mM 0.5134 mL 2.5668 mL 5.1336 mL
10 mM 0.2567 mL 1.2834 mL 2.5668 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.42 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.46%

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Keywords:

DalcetrapibJTT-705RO4607381JTT705JTT 705RO 4607381RO-4607381CETPCholesteryl ester transfer proteinInhibitorinhibitorinhibit

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Dalcetrapib
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HY-14950
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