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ChemicalBook >> CAS DataBase List >>Betrixaban

Betrixaban

CAS No.
330942-05-7
Chemical Name:
Betrixaban
Synonyms
CS-1417;MK-4448;PRT-021;MLN-1021;PRT 054021;Betrixaban;Bertixaban;Betrixaban-d4;Betrixaban, >=98%;Betrixaban USP/EP/BP
CBNumber:
CB02500171
Molecular Formula:
C23H22ClN5O3
Molecular Weight:
451.91
MDL Number:
MFCD16038040
MOL File:
330942-05-7.mol
MSDS File:
SDS
TDS File:
TDS
Last updated:2026-06-03 11:24:09
Product description Number Pack Size Price
Betrixaban ≥98% (HPLC) SML2845 5MG $104
Betrixaban ≥98% (HPLC) SML2845 25MG $420
Betrixaban B6398 250MG $196
Betrixaban ≥98% 21563 25mg $241
Betrixaban ≥98% 21563 50mg $362
More product size

Betrixaban Properties

Melting point 210-213°C
Density 1.30±0.1 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO (Slightly), Methanol (Slightly)
form Solid
pka 11.00±0.70(Predicted)
color Off-White
InChI InChI=1S/C23H22ClN5O3/c1-29(2)26-13-15-4-6-16(7-5-15)22(30)27-20-10-9-18(32-3)12-19(20)23(31)28-21-11-8-17(24)14-25-21/h4-14H,1-3H3,(H,27,30)(H,25,28,31)
InChIKey PGOYJYHMBCZDLN-UHFFFAOYSA-N
SMILES C(NC1=NC=C(Cl)C=C1)(=O)C1=CC(OC)=CC=C1NC(=O)C1=CC=C(C=NN(C)C)C=C1
CAS DataBase Reference 330942-05-7
FDA UNII 74RWP7W0J9
NCI Drug Dictionary betrixaban
ATC code B01AF04
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  Exclamation Mark (GHS07)Health Hazard (GHS08)
GHS07,GHS08
Signal word  Warning
Hazard statements  H302-H373
Precautionary statements  P301+P312+P330-P314
target organs Blood
WGK Germany  WGK 3
Storage Class 11 - Combustible Solids
Hazard Classifications Acute Tox. 4 Oral
STOT RE 2
NFPA 704
0
2 0

Betrixaban price More Price(89)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich SML2845 Betrixaban ≥98% (HPLC) 330942-05-7 5MG $104 2026-04-30 Buy
Sigma-Aldrich SML2845 Betrixaban ≥98% (HPLC) 330942-05-7 25MG $420 2026-04-30 Buy
TCI Chemical B6398 Betrixaban 330942-05-7 250MG $196 2026-04-30 Buy
Cayman Chemical 21563 Betrixaban ≥98% 330942-05-7 25mg $241 2026-04-30 Buy
Cayman Chemical 21563 Betrixaban ≥98% 330942-05-7 50mg $362 2026-04-30 Buy
Product number Packaging Price Buy
SML2845 5MG $104 Buy
SML2845 25MG $420 Buy
B6398 250MG $196 Buy
21563 25mg $241 Buy
21563 50mg $362 Buy

Betrixaban Chemical Properties,Uses,Production

Uses

Betrixaban is a novel anticoagulant, an oral direct inhibitor of factor Xa (FXa) for use in the prevention of venous thromboembolism (VTE).

Definition

ChEBI: Betrixaban is a secondary carboxamide obtained by formal condensation of the carboxy group of 4-(N,N-dimethylcarbamimidoyl)benzoic acid with the amino group of 2-amino-N-(5-chloropyridin-2-yl)-5-methoxybenzamide. A synthetic anticoagulant compound that targets activated factor Xa in the coagulation cascade. It has a role as an anticoagulant and an EC 3.4.21.6 (coagulation factor Xa) inhibitor. It is a member of guanidines, a member of benzamides, a secondary carboxamide, a monochloropyridine and a monomethoxybenzene.

Biological Activity

betrixaban is a highly potent, selective, and orally efficacious inhibitor of factor xa with ic50 value of 1.5nm [1].betrixaban shows excellent anticoagulant potency in vitro. in the rabbit deep vein thrombosis model, the concentration of betrixaban required to double the rabbit prothrombin time is below 2μm. betrixaban is selective for fxa and has poor activity for thrombin, trypsin, t-pa and apc. the patch clamp herg assay shows that betrixaban has low affinity with herg suggesting it is safer than other candidate compounds. in addition, betrixaban displays a profile of good oral bioavailability and oral exposure, long half-life in animal models. it has bioavailability of 51.6% at dose of 0.5 mg/kg iv and 2.5 mg/kg po. furthermore, the phase ii study has proved betrixaban as an oral fxa inhibitor for prevention of venous thromboembolic events [1].

in vivo

Betrixaban (0.5 mg/kg, i.v.; 2.5 mg/kg, p.o.) has oral bioavailability of 51.6% in dog[1].
Betrixaban (0.75 mg/kg, i.v.; 7.5 mg/kg, p.o.) has oral bioavailability of 58.7% in monkey[1].
Betrixaban mediated whole-blood INR increase is reversed by r-Antidote. After i.v. infusion for 30 min, the total plasma concentrations of Betrixaban is 0.2±0.01 μM, and the percentages of unbound inhibitor is 40%±7.2%. After administration of r-Antidote, the total plasma concentration increased to 2.0±0.4 μM, and the percentage of unbound inhibitor declined to 0.3%±0.1%[2].
Betrixaban (3 mg/kg) shows nearly comparable inhibition of thrombus mass to enoxaparin 1.6 mg/kg (76% vs 96% inhibition) in the rabbit abdominal vena cava model of clot accretion on cotton threads[3].
Betrixaban (19.1 mg/kg) is at least as effective at maintaining patency as enoxaparin 7.6 mg/kg and clopidogrel 3 mg/kg/d (90% vs 70% vs 80% patency, respectively) in the ferric chloride injury model of rodent carotid artery[3].

References

[1] 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.

88905-74-2
330942-01-3
330942-05-7
Synthesis of Betrixaban from Magnesium, chloro(N-methylmethanaminato)- (9CI) and N-(5-Chloro-2-pyridinyl)-2-[(4-cyanobenzoyl)amino]-5-methoxybenzamide

Betrixaban Preparation Products And Raw materials

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Dideu Industries Group Limited
+86-29-89586680 +86-15129568250 1026@dideu.com China 20582 58

View Lastest Price from Betrixaban manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Betrixaban pictures 2026-06-05 Betrixaban
330942-05-7
1g 98%min 1000g WUHAN FORTUNA CHEMICAL CO., LTD
Betrixaban pictures 2026-06-02 Betrixaban
330942-05-7
$39.00-97.00 99.35% 10g TargetMol Chemicals Inc.
Betrixaban USP/EP/BP pictures 2025-11-18 Betrixaban USP/EP/BP
330942-05-7
$1.10 1g 99.9% 100 Tons min Dideu Industries Group Limited
  • Betrixaban pictures
  • Betrixaban
    330942-05-7
  • $0.00
  • 98%min
  • WUHAN FORTUNA CHEMICAL CO., LTD
  • Betrixaban pictures
  • Betrixaban
    330942-05-7
  • $39.00-97.00
  • 99.35%
  • TargetMol Chemicals Inc.
Betrixaban N-(5-Chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide Betrixaban, >=98% Betrixaban, PRT-054021 1-C-{4-[aMino(diMethylaMino)Methyl]benzene}-2-N-(5-chloropyridin-2-yl)-4-Methoxybenzene-1,2-dicarboxaMide N-(5-Chloro-2-pyridinyl)-2-[[4-[(diMethylaMino)iMinoMethyl]benzoyl]aMino]-5-MethoxybenzaMide PRT 054021 N-(5-chloropyridin-2-yl)-2-(4-(N,N-diMethylcarbaMiMidoyl)benzaMido)-4-MethoxybenzaMide N-(5-CHLOROPYRIDIN-2-YL)-2-(4-(N,N-DIMETHYLCARBAMIMIDOYL)BENZAMIDO)-5-METHOXYBENZAMIDE Betrixaban N-(5-Chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide N-(5-Chloropyridin-2-yl)-2-[[4-(N,N-dimethylcarbamimidoyl)benzoyl]amino]-5-methoxybenzamide Betrixaban N-HYDROXY-4-PYRIDAZINECARBOXAMIDE Betrixaban-d4 CS-1417 BETRIXABAN;MK-4448; PRT-021; PRT-054021; MLN-1021 MK-4448 MLN-1021 PRT-021 N-(5-chloropyridin-2-yl)-2-({[4-(N,N-dimethylcarbamimidoyl)phenyl]carbonyl}amino)-5-methoxybenzamide Benzamide, N-(5-chloro-2-pyridinyl)-2-[[4-[(dimethylamino)iminomethyl]benzoyl]amino]-5-methoxy- Betrixaban USP/EP/BP Bertixaban N-(5-chloropyridin-2-yl)-2-({[4-(N,N-dimethylcarbamimidoyl)p... Betrixaban, 10 mM in DMSO Betrixaban - Bio-X ? 330942-05-7 API Aromatics Heterocycles Inhibitors Intermediates & Fine Chemicals Pharmaceuticals
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