Obicetrapib (free base)

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 327018

CAS#: 866399-87-3 (free base)

Description: Obicetrapib (also known as AMG-899, TA-8995, and DEX-001) is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.


Price and Availability

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Obicetrapib free base is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 327018
Name: Obicetrapib (free base)
CAS#: 866399-87-3 (free base)
Chemical Formula: C32H31F9N4O5
Exact Mass: 722.2151
Molecular Weight: 722.6086
Elemental Analysis: C, 53.19; H, 4.32; F, 23.66; N, 7.75; O, 11.07


Related CAS #: 866399-87-3 (free base)   866399-89-5 (calcium)    

Synonym: Obicetrapib; AMG-899; AMG 899; AMG899; TA-8995; TA8995; TA 8995; DEZ-001; DEZ 001; DEZ001.

IUPAC/Chemical Name: 4-((2-((3,5-bis(trifluoromethyl)benzyl)((2R,4S)-1-(ethoxycarbonyl)-2-ethyl-6-(trifluoromethyl)-1,2,3,4-tetrahydroquinolin-4-yl)amino)pyrimidin-5-yl)oxy)butanoic acid

InChi Key: NRWORBQAOQVYBJ-GJZUVCINSA-N

InChi Code: InChI=1S/C32H31F9N4O5/c1-3-22-14-26(24-13-19(30(33,34)35)7-8-25(24)45(22)29(48)49-4-2)44(28-42-15-23(16-43-28)50-9-5-6-27(46)47)17-18-10-20(31(36,37)38)12-21(11-18)32(39,40)41/h7-8,10-13,15-16,22,26H,3-6,9,14,17H2,1-2H3,(H,46,47)/t22-,26+/m1/s1

SMILES Code: O=C(O)CCCOC1=CN=C(N(CC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)[C@H]3C[C@@H](CC)N(C(OCC)=O)C4=C3C=C(C(F)(F)F)C=C4)N=C1


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

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


Additional Information

Related CAS#
866399-87-3 (free base); 866399-89-5 (calcium)


References

1: Filippatos TD, Klouras E, Barkas F, Elisaf M. Cholesteryl ester transfer protein inhibitors: challenges and perspectives. Expert Rev Cardiovasc Ther. 2016 Aug;14(8):953-62. doi: 10.1080/14779072.2016.1189327. Epub 2016 May 28. PubMed PMID: 27171534.

2: Amgen bulks out cardio package. Nat Biotechnol. 2015 Nov;33(11):1118. doi: 10.1038/nbt1115-1118a. PubMed PMID: 26544124.

3: Mearns BM. Dyslipidaemia: Promising results for TA-8995 in TULIP. Nat Rev Cardiol. 2015 Aug;12(8):443. doi: 10.1038/nrcardio.2015.97. Epub 2015 Jun 23. PubMed PMID: 26099844.

4: Hovingh GK, Kastelein JJ, van Deventer SJ, Round P, Ford J, Saleheen D, Rader DJ, Brewer HB, Barter PJ. Cholesterol ester transfer protein inhibition by TA-8995 in patients with mild dyslipidaemia (TULIP): a randomised, double-blind, placebo-controlled phase 2 trial. Lancet. 2015 Aug 1;386(9992):452-60. doi: 10.1016/S0140-6736(15)60158-1. Epub 2015 Jun 2. PubMed PMID: 26047975.

5: Ford J, Lawson M, Fowler D, Maruyama N, Mito S, Tomiyasu K, Kinoshita S, Suzuki C, Kawaguchi A, Round P, Boyce M, Warrington S, Weber W, van Deventer S, Kastelein JJ. Tolerability, pharmacokinetics and pharmacodynamics of TA-8995, a selective cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects. Br J Clin Pharmacol. 2014 Sep;78(3):498-508. doi: 10.1111/bcp.12380. PubMed PMID: 24628035; PubMed Central PMCID: PMC4243901.

6: Mousa SS, Block RC, Mousa SA. High Density Lipoprotein (HDL) Modulation Targets. Drugs Future. 2010 Jan;35(1):33-39. PubMed PMID: 22740724; PubMed Central PMCID: PMC3381456.