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CAS No.: 330942-05-7

Betrixaban/贝曲西班 Catalog No. CSN12369

Synonyms: PRT054021;MK-4448;PRT-021

Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM (inhibition of Factor 10a).

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实验方案

技术信息

生物活性

描述Serine protease factor Xa (fXa), positioned at the juncture of the intrinsic and the extrinsic pathways, play a pivotal role in the blood coagulation cascade ^[3]. Betrixaban is a highly potent, selective, and orally efficacious fXa inhibitor with IC50of 1.5 nM. In patch clamp hERG (human ether-a-go-go related gene) assays, Betrixaban has IC50 value of 8.9 μM. The plasma kallikrein IC50 and Ki values for Betrixaban are 6.3 μM and 3.5 μM respectively. Betrixaban (hERG Ki 1.8 μM) exhibits significantly lower hERG activity than all the others (hERG Ki⩽0.5 μM) ^[3]. Dosed at 0.5 mg/kg IV and 2.5 mg/kg PO, Betrixaban has bioavailability of 51.6% in dog; dosed at 0.75 mg/kg IV and 7.5 mg/kg PO, Betrixaban has bioavailability of 58.7% in monkey ^[3]. After i.v. infusion for 30 min, the total plasma concentration of Betrixaban is 0.2±0.01 μM, and the percentage of unbound inhibitor is 40%±7.2% ^[4].
作用机制The chloropyridine A ring extents into the fXa S1 site with the chloro atom positioned above the phenyl ring of Tyr228 and occupies a hydrophobic pocket formed by Ala190, Val213 and Tyr228.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT03728166	Venous Thromboembolism	Phase 4	Not yet recruiting	February 1, 2021	-
NCT03397888	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... more >> Clinical Pharmacology of Miami Hialeah, Florida, United States, 33014 Collapse <<
NCT03613402	-	-	Suspended(Due to slow enrollme... more >>nt.) Collapse <<	January 2020	United States, North Carolina ... more >> Durham Durham, North Carolina, United States, 27705 Collapse <<

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参考文献

[1] Lu G, DeGuzman FR, et al. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51.
[2] Zhang P, Huang W, et al. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenz amide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85.
[3] Zhang P, Huang W, Wang L, Bao L, Jia ZJ, Bauer SM, Goldman EA, Probst GD, Song Y, Su T, Fan J, Wu Y, Li W, Woolfrey J, Sinha U, Wong PW, Edwards ST, Arfsten AE, Clizbe LA, Kanter J, Pandey A, Park G, Hutchaleelaha A, Lambing JL, Hollenbach SJ, Scarborough RM, Zhu BY. Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2179-85. doi: 10.1016/j.bmcl.2009.02.111. Epub 2009 Mar 3. PMID: 19297154.
[4] Lu G, DeGuzman FR, Hollenbach SJ, Karbarz MJ, Abe K, Lee G, Luan P, Hutchaleelaha A, Inagaki M, Conley PB, Phillips DR, Sinha U. A specific antidote for reversal of anticoagulation by direct and indirect inhibitors of coagulation factor Xa. Nat Med. 2013 Apr;19(4):446-51. doi: 10.1038/nm.3102. Epub 2013 Mar 3. PMID: 23455714.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2129 mL
- 11.0643 mL
- 22.1285 mL
- 5 mM
- 0.4426 mL
- 2.2129 mL
- 4.4257 mL
- 10 mM
- 0.2213 mL
- 1.1064 mL
- 2.2129 mL

技术信息

CAS号

330942-05-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H22ClN5O3

运输

蓝冰

分子量

451.91

别名

PRT054021;MK-4448;PRT-021;MLN-1021;贝曲西班

溶解度

DMSO	59.0 mg/mL (130.6 mM) warming
Water	insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03728166	Venous Thromboembolism	Phase 4	Not yet recruiting	February 1, 2021	-
NCT03397888	Hepatic Impairment	Phase 1	Completed	-	United States, Florida ... more >> Clinical Pharmacology of Miami Hialeah, Florida, United States, 33014 Collapse <<
NCT03613402	-	-	Suspended(Due to slow enrollme... more >>nt.) Collapse <<	January 2020	United States, North Carolina ... more >> Durham Durham, North Carolina, United States, 27705 Collapse <<
NCT00375609	Thromboembolism	Phase 2	Completed	-	Canada, Quebec ... more >> Montreal General Hospital Montreal, Quebec, Canada, H3Y 3B8 Collapse <<
NCT00375609	-	-	Completed	-	-
NCT01229254	-	-	Completed	-	-
NCT03330457	Bleeding	Phase 2	Recruiting	September 2018	United States, California ... more >> WCCT Global Recruiting Cypress, California, United States, 90630 Contact 714-252-0700 Collapse <<
NCT01765855	Health Volunteers	Phase 1	Completed	-	-
NCT00742859	-	-	Completed	-	-
NCT00742859	Atrial Fibrillation	Phase 2	Completed	-	United States, California ... more >> Portola Investigational Site Anaheim, California, United States, 92801 United States, Colorado Portola Investigational Site Colorado Springs, Colorado, United States, 80909 United States, Florida Portola Investigational Site Melbourne, Florida, United States, 32901 Portola Investigational Site Miami, Florida, United States, 33173 Portola Investigational Site Ormond Beach, Florida, United States, 32174 Portola Investigational Site Pensacola, Florida, United States, 32501 Portola Investigational Site Port Charlotte, Florida, United States, 33952 United States, Illinois Portola Investigational Site Aurora, Illinois, United States, 60504 United States, Maine Portola Investigational Site Auburn, Maine, United States, 04210 United States, Maryland Portola Investigational Site Columbia, Maryland, United States, 21044 Portola Investigational Site Salisbury, Maryland, United States, 21804 Portola Investigational Site Towson, Maryland, United States, 21204 United States, Mississippi Portola Investigational Site Tupelo, Mississippi, United States, 38801 United States, Missouri Portola Investigational Site Saint Louis, Missouri, United States, 63110 United States, New York Portola Investigational Site Poughkeepsie, New York, United States, 12601 United States, Oregon Portola Investigational Site Hillsboro, Oregon, United States, 97123 United States, Pennsylvania Portola Investigational Site Wynnewood, Pennsylvania, United States, 19096 United States, South Dakota Portola Investigational Site Rapid City, South Dakota, United States, 57701 United States, Virginia Portola Investigational Site Norfolk, Virginia, United States, 23507 Canada, Quebec Portola Investigational Site Longueuil, Quebec, Canada Portola Investigational Site Montreal, Quebec, Canada Collapse <<
NCT01765868	Healthy Subjects	Phase 1	Completed	-	-
NCT03346083	VTE Prophylaxis	Phase 1	Recruiting	April 2022	Russian Federation ... more >> Children's Hospital of Tatarstan Republic Recruiting Kazan, Russian Federation Federal State Institution Recruiting Kemerovo, Russian Federation State Budgetary Institution Recruiting Nizhnii Novgorod, Russian Federation Federal State Budgetary Institution Recruiting Saint Petersburg, Russian Federation Collapse <<
NCT01229254	Atrial Fibrillation ... more >> Atrial Flutter Collapse <<	Phase 2	Completed	-	-
NCT00999336	Renal Impairment	Phase 1	Completed	-	Germany ... more >> APEX GmbH Munich, Germany Collapse <<
NCT01583218	Venous Thromboembolism (VTE)	Phase 3	Completed	-	-
NCT01583218	-	-	Completed	-	-
NCT02596100	Healthy	Phase 1	Completed	-	-

Betrixaban/贝曲西班 Catalog No. CSN12369

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