Dalcetrapib
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MedKoo CAT#: 319508

CAS#: 211513-37-0

Description: Dalcetrapib, aslo known as JTT-705, is a CETP inhibitor. The drug was aimed at raising the blood levels of "good cholesterol" (cholesterol carried in HDL particles, aka HDL-C). Prevailing observations indicate that high HDL levels correlate with better overall cardiovascular health, though it remains unclear whether raising HDL levels consequently leads to an increase in cardiovascular health. Development of this drug was halted on May 7, 2012 “due to a lack of clinically meaningful efficacy.


Price and Availability

Size
Price

5mg
USD 350
Size
Price

Size
Price

Dalcetrapib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 319508
Name: Dalcetrapib
CAS#: 211513-37-0
Chemical Formula: C23H35NO2S
Exact Mass: 389.23885
Molecular Weight: 389.598
Elemental Analysis: C, 70.91; H, 9.06; N, 3.60; O, 8.21; S, 8.23


Synonym: JTT-705; JTT705; JTT 705; RO-4607381; RO4607381; RO 4607381; Dalcetrapib.

IUPAC/Chemical Name: S-[2-[[1-(2-ethylbutyl)cyclohexanecarbonyl]amino]phenyl] 2-methylpropanethioate

InChi Key: YZQLWPMZQVHJED-UHFFFAOYSA-N

InChi Code: InChI=1S/C23H35NO2S/c1-5-18(6-2)16-23(14-10-7-11-15-23)22(26)24-19-12-8-9-13-20(19)27-21(25)17(3)4/h8-9,12-13,17-18H,5-7,10-11,14-16H2,1-4H3,(H,24,26)

SMILES Code: CC(C)C(SC1=CC=CC=C1NC(C2(CC(CC)CC)CCCCC2)=O)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Johns DG, Chen Y, Wang SP, Castro-Perez J, Previs SF, Roddy TP. Inhibition of cholesteryl ester transfer protein increases cholesteryl ester content of large HDL independently of HDL-to-HDL homotypic transfer: in vitro vs in vivo comparison using anacetrapib and dalcetrapib. Eur J Pharmacol. 2015 Sep 5;762:256-62. doi: 10.1016/j.ejphar.2015.05.061. Epub 2015 Jun 3. PubMed PMID: 26049012.

2: Tardif JC, Rhéaume E, Lemieux Perreault LP, Grégoire JC, Feroz Zada Y, Asselin G, Provost S, Barhdadi A, Rhainds D, L'Allier PL, Ibrahim R, Upmanyu R, Niesor EJ, Benghozi R, Suchankova G, Laghrissi-Thode F, Guertin MC, Olsson AG, Mongrain I, Schwartz GG, Dubé MP. Pharmacogenomic determinants of the cardiovascular effects of dalcetrapib. Circ Cardiovasc Genet. 2015 Apr;8(2):372-82. doi: 10.1161/CIRCGENETICS.114.000663. Epub 2015 Jan 11. PubMed PMID: 25583994.

3: Niesor EJ, Kallend D, Bentley D, Kastelein JJ, Kees Hovingh G, Stroes ES. Treatment of low HDL-C subjects with the CETP modulator dalcetrapib increases plasma campesterol only in those without ABCA1 and/or ApoA1 mutations. Lipids. 2014 Dec;49(12):1245-9. doi: 10.1007/s11745-014-3956-x. Epub 2014 Oct 4. PubMed PMID: 25281277.

4: Briand F, Thieblemont Q, Muzotte E, Burr N, Urbain I, Sulpice T, Johns DG. Anacetrapib and dalcetrapib differentially alters HDL metabolism and macrophage-to-feces reverse cholesterol transport at similar levels of CETP inhibition in hamsters. Eur J Pharmacol. 2014 Oct 5;740:135-43. doi: 10.1016/j.ejphar.2014.06.022. Epub 2014 Jul 5. PubMed PMID: 25008069.

5: Takubo H, Ishikawa T, Kuhlmann O, Nemoto H, Noguchi T, Nanayama T, Komura H, Kogayu M. Pharmacokinetics and disposition of dalcetrapib in rats and monkeys. Xenobiotica. 2014 Dec;44(12):1117-26. doi: 10.3109/00498254.2014.932471. Epub 2014 Jun 23. PubMed PMID: 24954481.

6: Tomoda H. Dalcetrapib in patients with an acute coronary syndrome. N Engl J Med. 2013 Feb 28;368(9):869. doi: 10.1056/NEJMc1300057#SA1. PubMed PMID: 23445099.

7: Schwartz GG, Olsson AG, Barter PJ. Dalcetrapib in patients with an acute coronary syndrome. N Engl J Med. 2013 Feb 28;368(9):869-70. doi: 10.1056/NEJMc1300057. PubMed PMID: 23445098.

8: Phelan M, Anzures-Cabrera J, Carlile DJ, Rowell L, Kuhlmann O, Arold G, Robson R, Bentley D. Effect of hepatic and renal impairment on the pharmacokinetics of dalcetrapib: altered distribution of the active thiol? Clin Pharmacokinet. 2013 Apr;52(4):255-65. doi: 10.1007/s40262-013-0035-z. PubMed PMID: 23400900.

9: Aceves Baldó P, Anzures-Cabrera J, Bentley D. In vivo evaluation of drug-drug interactions linked to UGT inhibition: the effect of probenecid on dalcetrapib pharmacokinetics. Int J Clin Pharmacol Ther. 2013 Mar;51(3):215-8. doi: 10.5414/CP201766. PubMed PMID: 23357838.

10: Lim GB. Lipids. Dalcetrapib raises HDL-cholesterol level, but does not reduce cardiac risk. Nat Rev Cardiol. 2013 Jan;10(1):5. doi: 10.1038/nrcardio.2012.171. Epub 2012 Nov 20. PubMed PMID: 23165074.

11: Schwartz GG, Olsson AG, Abt M, Ballantyne CM, Barter PJ, Brumm J, Chaitman BR, Holme IM, Kallend D, Leiter LA, Leitersdorf E, McMurray JJ, Mundl H, Nicholls SJ, Shah PK, Tardif JC, Wright RS; dal-OUTCOMES Investigators. Effects of dalcetrapib in patients with a recent acute coronary syndrome. N Engl J Med. 2012 Nov 29;367(22):2089-99. doi: 10.1056/NEJMoa1206797. Epub 2012 Nov 5. PubMed PMID: 23126252.

12: Goldberg AS, Hegele RA. Cholesteryl ester transfer protein inhibitors for dyslipidemia: focus on dalcetrapib. Drug Des Devel Ther. 2012;6:251-9. doi: 10.2147/DDDT.S34976. Epub 2012 Sep 24. Review. PubMed PMID: 23055695; PubMed Central PMCID: PMC3460676.

13: Gross G, Tardio J, Kuhlmann O. Solubility and stability of dalcetrapib in vehicles and biological media. Int J Pharm. 2012 Nov 1;437(1-2):103-9. doi: 10.1016/j.ijpharm.2012.07.071. Epub 2012 Aug 4. PubMed PMID: 22884829.

14: Rhainds D, Arsenault BJ, Brodeur MR, Tardif JC. An update on the clinical development of dalcetrapib (RO4607381), a cholesteryl ester transfer protein modulator that increases HDL cholesterol levels. Future Cardiol. 2012 Jul;8(4):513-31. doi: 10.2217/fca.12.25. Review. PubMed PMID: 22871191.

15: Hooper AJ, Burnett JR. Dalcetrapib , a cholesteryl ester transfer protein modulator. Expert Opin Investig Drugs. 2012 Sep;21(9):1427-32. doi: 10.1517/13543784.2012.699040. Epub 2012 Jun 24. PubMed PMID: 22725099.

16: Heinig K, Bucheli F, Kuhlmann O, Zell M, Pähler A, Zwanziger E, Gross G, Tardio J, Ishikawa T, Yamashita T. Determination of dalcetrapib by liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:314-24. doi: 10.1016/j.jpba.2012.03.056. Epub 2012 Apr 6. PubMed PMID: 22541249.

17: Young A, Anzures-Cabrera J, Derks M. No clinically relevant drug-drug interactions when dalcetrapib is co-administered with a monophasic oral contraceptive (Microgynon® 30). Int J Clin Pharmacol Ther. 2012 Apr;50(4):248-56. PubMed PMID: 22456295.

18: Ballantyne CM, Miller M, Niesor EJ, Burgess T, Kallend D, Stein EA. Effect of dalcetrapib plus pravastatin on lipoprotein metabolism and high-density lipoprotein composition and function in dyslipidemic patients: results of a phase IIb dose-ranging study. Am Heart J. 2012 Mar;163(3):515-21, 521.e1-3. doi: 10.1016/j.ahj.2011.11.017. PubMed PMID: 22424025.

19: Lim GB. Pharmacotherapy. Elevating HDL-cholesterol levels with dalcetrapib is safe. Nat Rev Cardiol. 2012 Mar 6;9(5):257. doi: 10.1038/nrcardio.2012.31. PubMed PMID: 22392063.

20: Lüscher TF, Taddei S, Kaski JC, Jukema JW, Kallend D, Münzel T, Kastelein JJ, Deanfield JE; dal-VESSEL Investigators. Vascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial. Eur Heart J. 2012 Apr;33(7):857-65. doi: 10.1093/eurheartj/ehs019. Epub 2012 Feb 16. PubMed PMID: 22345126; PubMed Central PMCID: PMC3345558.