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Razaxaban HCl_405940-76-3_产品详情
405940-76-3
  • names:

    1H-Pyrazole-5-carboxamide, 1-(3-amino-1,2-benzisoxazol-5-yl)-N-(4-(2-((dimethylamino)methyl)-1H-imidazol-1-yl)-2-fluorophenyl)-3-(trifluoromethyl)-, monohydrochloride

  • CAS号:

    405940-76-3

    MDL Number:
  • MF(分子式): C24H21ClF4N8O2 MW(分子量): 564.9296
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Razaxaban HCl
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中文别名 1H-Pyrazole-5-carboxamide, 1-(3-amino-1,2-benzisoxazol-5-yl)-N-(4-(2-((dimethylamino)methyl)-1H-imidazol-1-yl)-2-fluorophenyl)-3-(trifluoromethyl)-, monohydrochloride
英文别名 Razaxaban hydrochloride; BMS-561389; BMS-561389-01; DPC-906; BMS-561389-06; BMS561389; BMS561389-01; DPC906; BMS561389-06.
CAS号 405940-76-3
Inchi InChI=1S/C24H20F4N8O2.ClH/c1-34(2)12-21-30-7-8-35(21)13-3-5-17(16(25)10-13)31-23(37)18-11-20(24(26,27)28)32-36(18)14-4-6-19-15(9-14)22(29)33-38-19;/h3-11H,12H2,1-2H3,(H2,29,33)(H,31,37);1H
InchiKey CASCTHHMARGRLB-UHFFFAOYSA-N
分子式 Formula C24H21ClF4N8O2
分子量 Molecular Weight 564.9296
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 Razaxaban HCl(CAS:405940-76-3 ):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionRazaxaban, also known as BMS-561389; BMS-561389-01; DPC-906; BMS-561389-06, is a factor Xa inhibitor potentially for the treatment of thrombosis. Razaxaban was an effective antithrombotic agent in a rabbit model of arterial thrombosis. Low-dose razaxaban was useful in combination with sub-optimal doses of aspirin and/or clopidogrel for the prevention of occlusive arterial thrombosis without excessive bleeding.
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备注
[1]Badawy SI, Narang AS, LaMarche K, Subramanian G, Varia SA. Mechanistic basis for the effects of process parameters on quality attributes in high shear wet granulation. Int J Pharm. 2012 Dec 15;439(1-2):324-33. doi: 10.1016/j.ijpharm.2012.09.01[1]PubMed PMID: 22981985.
[2]Barrett YC, Wang Z, Knabb RM. A novel prothrombin time assay for assessing the anticoagulant activity of oral factor Xa inhibitors. Clin Appl Thromb Hemost. 2013 Sep;19(5):522-8. doi: 10.1177/1076029612441859. PubMed PMID: 22473028.
[3] Pugh N, Jarvis GE, Koch A, Sakariassen KS, Davis B, Farndale RW. The impact of factor Xa inhibition on axial dependent arterial thrombus formation triggered by a tissue factor rich surface. J Thromb Thrombolysis. 2012 Jan;33(1):6-15. doi: 10.1007/s11239-011-0658-6. PubMed PMID: 22120925.
[4] Barrett YC, Wang Z, Frost C, Shenker A. Clinical laboratory measurement of direct factor Xa inhibitors: anti-Xa assay is preferable to prothrombin time assay. Thromb Haemost. 2010 Dec;104(6):1263-71. doi: 10.1160/TH10-05-0328. PubMed PMID: 20978714.
[5] Quan ML, Pinto DJ, Rossi KA, Sheriff S, Alexander RS, Amparo E, Kish K, Knabb RM, Luettgen JM, Morin P, Smallwood A, Woerner FJ, Wexler RR. Phenyltriazolinones as potent factor Xa inhibitors. Bioorg Med Chem Lett. 2010 Feb 15;20(4):1373-7. doi: 10.1016/j.bmcl.2010.01.011. PubMed PMID: 20100660.
6: Bátorová A. [Advances in antithrombotic treatment--antithrombotics with anti-Xa effect]. Vnitr Lek. 2009 Mar;55(3):295-301. Review. Slovak. PubMed PMID: 19378862.7: Hilden LR, Pommier CJ, Badawy SI, Friedman EM. NIR chemical imaging to guide/support BMS-561389 tablet formulation development. Int J Pharm. 2008 Apr 2;353(1-2):283-90. doi: 10.1016/j.ijpharm.2007.11.032. PubMed PMID: 18182257.8: Varnes JG, Wacker DA, Pinto DJ, Orwat MJ, Theroff JP, Wells B, Galemo RA, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR. Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors. Bioorg Med Chem Lett. 2008 Jan 15;18(2):749-54. PubMed PMID: 18054227.9: Zhang D, Raghavan N, Chen SY, Zhang H, Quan M, Lecureux L, Patrone LM, Lam PY, Bonacorsi SJ, Knabb RM, Skiles GL, He K. Reductive isoxazole ring opening of the anticoagulant razaxaban is the major metabolic clearance pathway in rats and dogs. Drug Metab Dispos. 2008 Feb;36(2):303-15. PubMed PMID: 17984286.10: Varnes JG, Wacker DA, Jacobson IC, Quan ML, Ellis CD, Rossi KA, He MY, Luettgen JM, Knabb RM, Bai S, He K, Lam PY, Wexler RR. Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors. Bioorg Med Chem Lett. 2007 Dec 1;17(23):6481-8. PubMed PMID: 17933529.1
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