Argatroban
Title: Argatroban
CAS Registry Number: 74863-84-6
CAS Name: (2R,4R)-1-[(2S)-5-[(Aminoiminomethyl)amino]-1-oxo-2-[[(1,2,3,4-tetrahydro-3-methyl-8-quinolinyl)sulfonyl]amino]pentyl]-4-methyl-2-piperidinecarboxylic acid
Additional Names: (2R,4R)-4-methyl-1-[N2-(3-methyl-1,2,3,4-tetrahydro-8-quinolinesulfonyl)-L-arginyl]-2-piperidinecarboxylic acid; (2R,4R)-4-methyl-1-[(S)-N2-[[(R,S)-1,2,3,4-tetrahydro-3-methyl-8-quinolinyl]sulfonyl]arginyl]pipecolic acid; argipidine; MQPA
Molecular Formula: C23H36N6O5S
Molecular Weight: 508.63
Percent Composition: C 54.31%, H 7.13%, N 16.52%, O 15.73%, S 6.30%
Literature References: Synthetic thrombin inhibitor. Prepn of argatroban and stereoisomers: R. Kikumoto et al., EP 8746; S. Okamoto et al., US 4258192 (1980, 1981 both to Mitsubishi Chem. Ind.); S. Okamoto et al., Biochem. Biophys. Res. Commun. 101, 440 (1981). Comparison with heparin, q.v., of antithrombotic effect in animals: T. Kumada, Y. Abiko, Thromb. Res. 24, 285 (1981). Stereoselective inhibition of thrombin: R. Kikumoto et al., Biochemistry 23, 85 (1984). Clinical evaluation in hemodialysis: K. Ota et al., Proc. Eur. Dial. Transplant. Assoc. 20, 144 (1983); in disseminated intravascular coagulation: K. Kumon et al., Crit. Care Med. 12, 1039 (1984).
Properties: Crystals from ethanol, mp 188-191°.
Melting point: mp 188-191°
 
Derivative Type: Monohydrate
CAS Registry Number: 141396-28-3
Manufacturers' Codes: DK-7419; MCI-9038; MD-805; OM-805
Trademarks: Novastan (Tokyo Tanabe); Slonnon (Daiichi)
Properties: Crystals from aq ethanol, mp 176-180°. [a]D27 +76.1° (c = 1 in 0.2N HCl).
Melting point: mp 176-180°
Optical Rotation: [a]D27 +76.1° (c = 1 in 0.2N HCl)
 
Therap-Cat: Antithrombotic.
Keywords: Antithrombotic.

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