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.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Obicetrapib |
|---|---|
| Iupac 化学名称 | 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 |
| 同义词 | Obicetrapib; AMG-899; AMG 899; AMG899; TA-8995; TA8995; TA 8995; DEZ-001; DEZ 001; DEZ001. |
| 英文同义词 | Obicetrapib; AMG-899; AMG 899; AMG899; TA-8995; TA8995; TA 8995; DEZ-001; DEZ 001; DEZ001. |
| 分子式 | C32H31F9N4O5 |
| 分子量 | 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号 | 866399-87-3 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
| 海关编码 |
| Targets | |
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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.
