Argatroban monohydrate

• CAT Number: I001576
• CAS Number: 141396-28-3
• Purity: ≥95%
• Synonyms: (2R,4R)-1-[(2S)-5-(diaminomethylideneamino)-2-[(3-methyl-1,2,3,4-tetrahydroquinolin-8-yl)sulfonylamino]pentanoyl]-4-methylpiperidine-2-carboxylic acid;hydrate
• InChI: InChI=1S/C23H36N6O5S.H2O/c1-14-8-10-29(18(12-14)22(31)32)21(30)17(6-4-9-26-23(24)25)28-35(33,34)19-7-3-5-16-11-15(2)13-27-20(16)19;/h3,5,7,14-15,17-18,27-28H,4,6,8-13H2,1-2H3,(H,31,32)(H4,24,25,26);1H2/t14-,15?,17+,18-;/m1./s1
• InChIKey: AIEZTKLTLCMZIA-CZSXTPSTSA-N
• SMILES: CC1CCN(C(C1)C(=O)O)C(=O)C(CCCN=C(N)N)NS(=O)(=O)C2=CC=CC3=C2NCC(C3)C.O

Argatroban (monohydrate) (MD-805 (monohydrate)) is a direct, selective thrombin inhibitor.
Argatroban (MD-805) may have a complementary effect for preventing thrombus formation without aggravating bleeding tendency because of its monotarget specificity to thrombin. Administration (0.5 to 2 micrograms/kg/min) of Argatroban (MD-805) is a safe anticoagulant for left heart bypass in repairs of traumatic aortic rupture associated with multiple organ injuries[1]. Argatroban (MD-805), as compared with heparin, appears to enhance reperfusion with TPA in patients with AMI, particularly in those patients with delayed presentation. The incidences of major bleeding and adverse clinical outcome were lower in the patients receiving argatroban[2].
Argatroban monohydrate can be used in animal modeling to construct endogenous intestinal plug models. Area under the curve values, distribution, and elimination half-life were significantly increased in hepatectomized rats. Argatroban is converted from the 21-(R) to the 21-(S) diastereomer in the kidney. The 21-(S) diastereomer has greater antithrombotic activity than the R isoform, and the 21-(S) isomer may be preferentially eliminated by the liver[4] .
Induction of Thrombolysis[3]
Background

Argatroban is a specific thrombin inhibitor that inhibits thrombin activity in animals to establish thrombolysis models.
Specific Mmodeling Methods

Rat: Wistar ST • male • 8-week-old 8
Administration: 2 mg/kg/h • iv • 1 h

Note

Rats were allowed drinking water ad libitum and were fasted overnight prior to the thrombolysis experiments.
Modeling Indicators

Relative rate of thrombus dissolution ↓
Correlated Product(s): Tranexamic acid (HY-B0149)
Opposite Product(s):