WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H578670
CAS#: 866399-89-5 (calcium)
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. TA-8995 dose dependently increased not only total and non-ABCA1-specific CEC but also ABCA1-specific CEC and preBeta-1 HDL particle levels.
Hodoodo Cat#: H578670
Name: Obicetrapib calcium
CAS#: 866399-89-5 (calcium)
Chemical Formula: C64H60CaF18N8O10
Exact Mass: 1,482.38
Molecular Weight: 1,483.280
Elemental Analysis: C, 51.82; H, 4.08; Ca, 2.70; F, 23.06; N, 7.55; O, 10.79
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 866399-87-3 (free acid) 866399-89-5 (calcium) 866399-88-4 (sodium) 866399-90-8 (potassium)
Synonym: Obicetrapib calcium; Obicetrapib; AMG-899; AMG 899; AMG899; TA-8995; TA8995; TA 8995; DEZ-001; DEZ 001; DEZ001;
IUPAC/Chemical Name: calcium 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)butanoate
InChi Key: QJYLTBPMVPTRPX-NVRNJZRHSA-L
InChi Code: InChI=1S/2C32H31F9N4O5.Ca/c2*1-3-22-14-26(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;/h2*7-8,10-13,15-16,22,26H,3-6,9,14,17H2,1-2H3,(H,46,47);/q;;+2/p-2/t2*22-,26+;/m11./s1
SMILES Code: [Ca+2].CCOC(=O)N1[C@H](CC)C[C@H](N(Cc2cc(cc(c2)C(F)(F)F)C(F)(F)F)c3ncc(OCCCC(=O)[O-])cn3)c4cc(ccc14)C(F)(F)F.CCOC(=O)N5[C@H](CC)C[C@H](N(Cc6cc(cc(c6)C(F)(F)F)C(F)(F)F)c7ncc(OCCCC(=O)[O-])cn7)c8cc(ccc58)C(F)(F)F
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 1,483.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Martin SS, Ditmarsch M, Simmons M, Alp N, Turner T, Davidson MH, Kastelein JJP. Comparison of low-density lipoprotein cholesterol equations in patients with dyslipidaemia receiving cholesterol ester transfer protein inhibition. Eur Heart J Cardiovasc Pharmacother. 2023 Feb 2;9(2):148-155. doi: 10.1093/ehjcvp/pvac056. PMID: 36307922; PMCID: PMC9892865.
2: Taheri H, Filion KB, Windle SB, Reynier P, Eisenberg MJ. Cholesteryl Ester Transfer Protein Inhibitors and Cardiovascular Outcomes: A Systematic Review and Meta-Analysis of Randomized Controlled Trials. Cardiology. 2020;145(4):236-250. doi: 10.1159/000505365. Epub 2020 Mar 13. PMID: 32172237.
3: Hey SP, Franklin JM, Avorn J, Kesselheim AS. Success, Failure, and Transparency in Biomarker-Based Drug Development: A Case Study of Cholesteryl Ester Transfer Protein Inhibitors. Circ Cardiovasc Qual Outcomes. 2017 Jun;10(6):e003121. doi: 10.1161/CIRCOUTCOMES.116.003121. PMID: 28611186.
4: Murín J, Pernický M, Kiňová S. Prístup k liečbe dyslipidémií - je tu ešte miesto pre CETP-inhibítory? [Treatment of dyslipidemia - is here still place for CETP-inhibitors?]. Vnitr Lek. 2016 Fall;62(10):789-794. Czech. PMID: 27900865.
5: van Capelleveen JC, Kastelein JJ, Zwinderman AH, van Deventer SJ, Collins HL, Adelman SJ, Round P, Ford J, Rader DJ, Hovingh GK. Effects of the cholesteryl ester transfer protein inhibitor, TA-8995, on cholesterol efflux capacity and high-density lipoprotein particle subclasses. J Clin Lipidol. 2016 Sep- Oct;10(5):1137-1144.e3. doi: 10.1016/j.jacl.2016.06.006. Epub 2016 Jun 25. PMID: 27678430.
6: 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. PMID: 27171534.
7: Amgen bulks out cardio package. Nat Biotechnol. 2015 Nov;33(11):1118. doi: 10.1038/nbt1115-1118a. PMID: 26544124.
8: 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. PMID: 26099844.
9: 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. PMID: 26047975.
10: 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. PMID: 24628035; PMCID: PMC4243901.
11: Mousa SS, Block RC, Mousa SA. High Density Lipoprotein (HDL) Modulation Targets. Drugs Future. 2010 Jan;35(1):33-39. doi: 10.1358/dof.2010.035.01.1452012. PMID: 22740724; PMCID: PMC3381456.
