Obicetrapib
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.
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Chemical Information
| Name | Obicetrapib |
|---|---|
| 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 |
| Synonyms | Obicetrapib; AMG-899; AMG 899; AMG899; TA-8995; TA8995; TA 8995; DEZ-001; DEZ 001; DEZ001. |
| Molecular Formula | C32H31F9N4O5 |
| Molecular Weight | 722.60 |
| Smile | 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 |
| InChiKey | NRWORBQAOQVYBJ-GJZUVCINSA-N |
| InChi | 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 |
| CAS Number | 866399-87-3 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | 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 |
| Handling | |
| 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. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
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.
Chemical Structure
