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75889-62-2
  • names:

    diethyl (4-(benzo[d]thiazol-2-yl)benzyl)phosphonate

  • CAS号:

    75889-62-2

    MDL Number:
  • MF(分子式): C18H20NO3PS MW(分子量): 361.3958
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Fostedil
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中文别名 Fostedil
英文别名 KB-944; KB 944; KB944; A 53986; A-53986; BRN 3626546; Fostedil
CAS号 75889-62-2
SMILES O=P(CC1=CC=C(C2=NC3=CC=CC=C3S2)C=C1)(OCC)OCC
Inchi InChI=1S/C18H20NO3PS/c1-3-21-23(20,22-4-2)13-14-9-11-15(12-10-14)18-19-16-7-5-6-8-17(16)24-18/h5-12H,3-4,13H2,1-2H3
InchiKey FVYRUSCZCWSFLT-UHFFFAOYSA-N
分子式 Formula C18H20NO3PS
分子量 Molecular Weight 361.3958
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
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 Fostedil(CAS:75889-62-2):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。
IntroductionFostedil, also known as KB-944, is a calcium channel antagonist potentially for the treatment of angina pectoris. KB-944 increased regional segment function in normal and ischemic regions and maintained distal coronary artery perfusion pressure, coronary flow and transmural regional myocardial blood flow during partial coronary artery occlusion despite a reduction in aortic pressure. In a model of total coronary artery occlusion.
Application1
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危险性 Warning
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安全声明
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[1]Sekine Y, Hirakawa N, Kashiwaba N, Matsumoto H, Kutsuma T, Yamaura T, Sekine A. A novel histamine 2(H2) receptor antagonist with gastroprotective activity. I. Synthesis and pharmacological evaluation of N-phenoxypropylacetamide derivatives with thioether function. Chem Pharm Bull (Tokyo). 1998 Apr;46(4):610-5. PubMed PMID: 9579036.
[2]Tchani G, Baziard-Mouysset G, Stigliani JL, Payard M, Bonnafous R, Tisne-Versailles J. Influence of the vinyl group on the calcium antagonistic activity of analogues of Fostedil. Pharm Acta Helv. 1994 Jan;68(3):173-9. PubMed PMID: 8121926.
[3] Rose U. [2-Aryl substituted benzo-anellated 5-ring-heterocycles as potential agents for the cardiovascular system. 2. 1,3-Benzimidazoles]. Pharmazie. 1991 Nov;46(11):775-7. German. PubMed PMID: 1811227.
[4] Staudinger R, Knaus HG, Glossmann H. Positive heterotropic allosteric regulators of dihydropyridine binding increase the Ca2+ affinity of the L-type Ca2+ channel. Stereoselective reversal by the novel Ca2+ antagonist BM 20.1140. J Biol Chem. 1991 Jun 15;266(17):10787-95. PubMed PMID: 1645709.
[5] Mouysset G, de Saqui-Sannes G, Younes S, Bellan J, Payard M, Tisne-Versailles J. Contribution of the diethyl phosphonate group to a first approach of calcium-inhibiting activity: study of a series of various substituted 2-phenylbenzothiazoles. Farmaco. 1990 Sep;45(9):945-52. PubMed PMID: 2282126.
6: Yoshino K, Goto K, Yoshiizumi K, Morita T, Tsukamoto G. Organic phosphorus compounds. 5. (4-Benzothiazol-2-ylbenzyl)amidophosphonate as potent calcium antagonistic vasodilators. J Med Chem. 1990 Aug;33(8):2192-6. PubMed PMID: 2374146.7: Yoshino K, Goto K, Kohno T, Morita T, Tsukamoto G. Organic phosphorus compounds. IV. Asymmetric 4-(benzothiazol-2-yl)benzylphosphonates as potent calcium antagonistic vasodilators. Chem Pharm Bull (Tokyo). 1990 Mar;38(3):676-80. PubMed PMID: 2347009.8: Bellucci C, Gualtieri F, Scapecchi S, Teodori E, Budriesi R, Chiarini A. Negative inotropic and calcium antagonistic activity of alkyl and arylalkyl phosphonates. Farmaco. 1989 Dec;44(12):1167-91. PubMed PMID: 2634406.9: Yoshino K, Kohno T, Morita T, Tsukamoto G. Organic phosphorus compounds. 2. Synthesis and coronary vasodilator activity of (benzothiazolylbenzyl) phosphonate derivatives. J Med Chem. 1989 Jul;32(7):1528-32. PubMed PMID: 2738888.10: Chiarini A, Valenti P, Fabbri G, da Re P. Chromosome and xanthone derivatives related to Fostedil. Acta Pharm Suec. 1987;24(5):257-62. PubMed PMID: 3450191.1
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