[CAS NO. 211513-37-0] Dalcetrapib
PRODUCTS SPECIFICATIONS [211513-37-0]
DESCRIPTION [211513-37-0]
Overview
| MDL | MFCD06407886 |
|---|---|
| Molecular Weight | 389.59 |
| Molecular Formula | C23H35NO2S |
| SMILES | CC(C)C(SC1=C(NC(C2(CC(CC)CC)CCCCC2)=O)C=CC=C1)=O |
Summary
In Vitro
In Vivo
Dalcetrapib (JTT-705) (30 or 100 mg/kg; p.o.; once a day for 3 days) increases plasma HDL cholesterol in rabbits
[2]
.
Dalcetrapib (100 mg/kg; i.g.; twice daily for 7 days) significantly increases fecal elimination of neutral sterols, bile acids, and plasma HDL-cholesterol
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male JW rabbits [2] |
| Dosage: | 30 or 100 mg/kg |
| Administration: | Oral administration, once a day for 3 days |
| Result: | Increased plasma HDL cholesterol by 27% and 54% at 30 mg/kg and 100 mg/kg, respectively. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT01476267 | Hoffmann-La Roche |
Healthy Volunteer
|
October 2011 | Phase 1 |
| NCT01323153 | Hoffmann-La Roche |
Coronary Heart Disease
|
March 2011 | Phase 3 |
| NCT00697203 | Hoffmann-La Roche |
Dyslipidemia
|
July 2005 | Phase 2 |
| NCT01059682 | Hoffmann-La Roche |
Cardiovascular Disease
|
January 2010 | Phase 3 |
| NCT01363999 | Hoffmann-La Roche |
Healthy Volunteer
|
June 2011 | Phase 1 |
| NCT00658515 | Hoffmann-La Roche |
Coronary Heart Disease
|
April 2008 | Phase 3 |
| NCT00689442 | Akros Pharma Inc. |
Dyslipidemia
|
January 2004 | Phase 2 |
| NCT00688558 | Akros Pharma Inc. |
Dyslipidemia
|
February 2004 | Phase 2 |
| NCT00655538 | Hoffmann-La Roche |
Coronary Heart Disease
|
February 2008 | Phase 2 |
| NCT04676867 | DalCor Pharmaceuticals|The Montreal Health Innovations Coordinating Center (MHICC)|Covance |
Covid19
|
January 11, 2021 | Phase 2 |
| NCT01516541 | Hoffmann-La Roche |
Cardiovascular Disease, Coronary Heart Disease, Dyslipidemia, Peripheral Arterial Disease (PAD)
|
January 2012 | Phase 3 |
| NCT00686010 | Japan Tobacco Inc. |
Type II Hyperlipidaemia
|
May 2000 | Phase 2 |
| NCT00353522 | Hoffmann-La Roche |
Coronary Heart Disease
|
July 2006 | Phase 2 |
| NCT00688896 | Akros Pharma Inc. |
Type II Hyperlipidemia
|
June 2002 | Phase 2 |
| NCT00655473 | Hoffmann-La Roche |
Coronary Heart Disease
|
March 2008 | Phase 2 |
| NCT02525939 | DalCor Pharmaceuticals|The Montreal Health Innovations Coordinating Center (MHICC)|Medpace, Inc.|Roche Molecular Systems, Inc |
Acute Coronary Syndrome
|
April 2016 | Phase 3 |
| NCT00400439 | Hoffmann-La Roche |
Coronary Heart Disease
|
January 2007 | Phase 2 |
Appearance
Solid
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
DMSO : ≥ 50 mg/mL ( 128.34 mM )
* "≥" means soluble, but saturation unknown.
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 |
References
- [1] Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51(12), 3443-3454.
- [2] Shinkai H, et al. J Med Chem. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. 2000, 43(19), 3566-3572.
- [3] Huang Z, et al. Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells. Am J Physiol Endocrinol Metab. 2003, 284(6), E1210-E1219.
Synonyms