Cilostazol 西洛他唑

CAS 73963-72-1 MFCD08063421

化学结构图

73963-72-1
SMILES: [2H]C1([2H])CCCC([2H])([2H])C1n1nnnc1CCCCOc1ccc2c(c1)CCC(=O)N2

化学属性

Mol. FormulaC20H27N5O2
Mol. Weight369
Melting Point158.0-162.0

别名和识别编码

Chemical NameCilostazol
CAS Number73963-72-1
Synonym 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-2(1H)-quinolinone
Beilstein Registry Number3632107
Chemical Name Translation西洛他唑
MDL NumberMFCD00866780
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分类

  • Pharmaceuticals
  • Intermediates & Fine Chemicals,

产品应用

  • A potent phosphodiesterase III A (PDE3A) inhibitor (IC50=0.2uM) and inhibitor of adenosine uptake. Has antimitogeni, antithrombotic, vasodilatory and cardiotonic properties in vivo. Also affects lip

相关文献及参考

  • [2]. Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo. Life Sci. 1997;61(25):PL 383-9.
  • [3]. Saito S, et al. Cilostazol attenuates hepatic stellate cell activation and protects mice against carbon tetrachloride-induced liver fibrosis. Hepatol Res. 2013 Apr 19.
  • [4]. Ye YL,et al. Cilostazol, a phosphodiesterase 3 inhibitor, protects mice against acute and late ischemic brain injuries.Eur J Pharmacol. 2007 Feb 14;557(1):23-31. Epub 2006 Nov 10.
  • Park, S.-W., et al.: Am. J. Cardiol., 84, 511 (1999),
  • Suri, A., et al.: J. Clin. Pharmacol., 38, 144 (1998),
  • Tsuchikane, E., et al.: Circulation, 100, 21 (1999),
  • [1]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9.
  • [1]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9.
  • [2]. Minami N

安全信息

RTECSVC8277500
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intramuscular
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : >1 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: -,504,1990

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >2 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: -,504,1990

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - man
DOSE/DURATION           : 1248 ug/kg
TOXIC EFFECTS :
   Behavioral - headache
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 35,1173,1985

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >5 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intramuscular
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : >1 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: -,504,1990

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 11 gm/kg
SEX/DURATION            : female 7-17 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Specific Developmental Abnormalities - skin and skin
   appendages
   Reproductive - Specific Developmental Abnormalities - cardiovascular
   (circulatory) system
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
REFERENCE :
   IYKEDH Iyakuhin Kenkyu.  Study of Medical Supplies.  (Nippon Koteisho
   Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan)  V.1- 1970- 
   Volume(issue)/page/year: 16,1053,1985

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 1650 mg/kg
SEX/DURATION            : female 17-22 day(s) after conception
                          lactating female 26 day(s) post-birth
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
REFERENCE :
   IYKEDH Iyakuhin Kenkyu.  Study of Medical Supplies.  (Nippon Koteisho
   Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan)  V.1- 1970- 
   Volume(issue)/page/year: 16,1073,1985

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 5250 mg/kg
SEX/DURATION            : female 5 week(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Maternal Effects - ovaries, fallopian tubes
   Reproductive - Maternal Effects - uterus, cervix, vagina
REFERENCE :
   IYKEDH Iyakuhin Kenkyu.  Study of Medical Supplies.  (Nippon Koteisho
   Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan)  V.1- 1970- 
   Volume(issue)/page/year: 16,1204,1985

TYPE OF TEST            : TD

GHS Symbol
WGK Germany2

系列性分类


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