Ketoconazole 酮康唑

规格: 98%
CAS: 65277-42-1
产品编号: H98013
MDL: MFCD00058579
品牌: INFI
Chemical NamePiperazine, 1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-, cis-
MDL NumberMFCD00058579
CAS Number65277-42-1
Synonym (±)-cis-1-Acetyl-4-(4-[(2-[2,4-dichlorophenyl]-2-[1H-imidazol-1-ylmethyl]-1,3-dioxolan-4-yl)-methoxy]phenyl)piperazine ()-cis-1-Acetyl-4-(4-[(2-[2,4-dichlorophenyl]-2-[1H-imidazol-1-ylmethyl]-1,3-dioxolan-4-yl)-methoxy]phenyl)piperazine (±)-cis-​1-​Acetyl-​4-​(4-​[(2-​[2,4-​dichlorophenyl]​-​2-​[1H-​imidazol-​1-​ylmethyl]​-​1,3-​dioxolan-​4-​yl)​-​methoxy]​phenyl)​piperazine Fungarest KW-1414 Ketoconazol Ketoderm Nizoral Orifungal M Panfungol R 41400
PubChem Substance ID87560321
EC Number265-667-4
Merck Number5302
Reaxys-RN5488107
Chemical Name Translation顺-1-乙酰基-4-[4-[[2-(2,4-二氯苯基)-2-(1H-咪唑-1-基甲基)-1,3-二氧戊环-4-基]甲氧基]苯基]哌嗪
Beilstein Registry Number5488107
Wiswesser Line NotationT6N DNTJ AV1 DR DO1- DT5O COTJ BR BG DG& B1- AT5N CNJ
LabNetwork Molecule IDLN01294533
GHS Symbol
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - guinea pig
DOSE/DURATION           : 23300 ug/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   MDACAP Medicamentos de Actualidad.  (J.R. Prous, S.A., Apartado de Correos
   540, 08080 Barcelona, Spain)  V.1-    1965-  Volume(issue)/page/year:
   17,373,1981

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 23300 ug/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   MDACAP Medicamentos de Actualidad.  (J.R. Prous, S.A., Apartado de Correos
   540, 08080 Barcelona, Spain)  V.1-    1965-  Volume(issue)/page/year:
   17,373,1981

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - guinea pig
DOSE/DURATION           : 178 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   MDACAP Medicamentos de Actualidad.  (J.R. Prous, S.A., Apartado de Correos
   540, 08080 Barcelona, Spain)  V.1-    1965-  Volume(issue)/page/year:
   17,373,1981

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 86 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   DRUGAY Drugs. International Journal of Current Therapeutics and Applied
   Pharmacology Reviews.  (ADIS Press International Inc., Suite B-30, Oxford
   Ct. Business Center, 582 Middletown Blvd., Langhorne, PA 19047)  V.1- 1971- 
   Volume(issue)/page/year: 23,1,1982

TYPE OF TEST

TYPE OF TEST            : DNA inhibition
TEST SYSTEM             : Human Cells - not otherwise specified
DOSE/DURATION           : 1 umol/L
REFERENCE :
   TUMOAB Tumori.  (Casa Editrice Ambrosiana, Via G. Frua 6, 20146 Milan,
   Italy)  V.1-    1911-  Volume(issue)/page/year: 77,385,1991

TYPE OF TEST            : DNA inhibition
TEST SYSTEM             : Human Lymphocyte
DOSE/DURATION           : 10 mg/L
REFERENCE :
   AMACCQ Antimicrobial Agents and Chemotherapy.  (American Soc. for
   Microbiology, 1913 I St., NW, Washington, DC 20006)  V.1-    1972-
   Volume(issue)/page/year: 24,478,1983

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 6480 mg/kg
SEX/DURATION            : male 9 week(s) pre-mating
                          female 2 week(s) pre-mating  - 7 day(s) after
                          conception
TOXIC EFFECTS :
   Reproductive - Fertility - mating performance (e.g. # sperm positive females
   per # females mated; # copulations per # estrus cycles)
   Reproductive - Fertility - female fertility index (e.g. # females pregnant
   per # sperm positive females; # females pregnant per # females mated)
REFERENCE :
   KSRNAM Kiso to Rinsho.  Clinical Report.  (Yubunsha Co., Ltd., 1-5, Kanda
   Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan)  V.1-    1960-
   Volume(issue)/page/year: 18,1433,1984

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - man
DOSE                    : 1029 mg/kg
SEX/DURATION            : male 60 day(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Paternal Effects - other effects on male
   Endocrine - androgenic
REFERENCE :
   ACENA7 Acta Endocrinologica (Copenhagen).  (Periodica, Skolegade 12 E,
   DK-2500 Valby, Denmark) V.1-    1948-  Volume(issue)/page/year: 110,276,1985

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 600 mg/kg
SEX/DURATION            : male 3 day(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Paternal Effects - spermatogenesis (incl. genetic material,
   sperm morphology, motility, and count)
   Reproductive - Fertility - male fertility index (e.g. # males impregnating
   females per # males exposed to fertile nonpregnant females)
REFERENCE :
   CCPTAY Contraception.  (Geron-X, Inc., POB 1108, Los Altos, CA 94022)  V.1-
   1970-  Volume(

WGK Germany3
Hazard statements
  • H301 Toxic if swallowed 吞食有毒
  • H360 May damage fertility or the unborn child 可能对生育能力或未出生婴儿造成伤害
  • H410 Verytoxictoaquaticlifewithlonglastingeffects 对水生生物毒性非常大并具有长期影响。
  • H373 May causes damage to organs through prolonged or repeated exposure 长期或频繁接触可能会损伤器官
    Personal Protective Equipment Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
    RTECSTK7912300
    Precautionary statements
    • P201 Obtain special instructions before use. 使用前获取专门指示。
    • P264 Wash hands thoroughly after handling. 处理后要彻底洗净双手。
    • P270 Do not eat, drink or smoke when using this product. 使用本产品时不要吃东西,喝水或吸烟。
    • P273 Avoid release to the environment. 避免释放到环境中。
    • P301+P310
    • P301+P310+P330
    • P308+P313
    • P405 Store locked up. 上锁保管。
    • P501 Dispose of contents/container to..… 处理内容物/容器.....
      Signal word Danger
      Safety Statements
      • S45 In case of accident or if you feel unwell seek medical advice immediately (show the label where possible) 发生事故时或感觉不适时,立即求医(可能时出示标签);
      • S53 Avoid exposure - obtain special instructions before use 避免接触,使用前获得特别指示说明;
      • S60 This material and its container must be disposed of as hazardous waste 该物质及其容器必须作为危险废物处置;
      • S61 Avoid release to the environment. Refer to special instructions/safety data sheet 避免释放到环境中,参考特别指示/安全收据说明书;
        Hazard Codes 6.1 T,N
        Risk Statements
        • R25 Toxic if swallowed 吞咽有毒
        • R48/22
        • R50/53
        • R60 May impair fertility 可能降低生殖能力
          Packing GroupIII
          UN Number 2811
          Storage condition 0-10 0-10°C
          Hazard Class6.1
        • {MCE} [2]. Eil C. Ketoconazole binds to the human androgen receptor. Horm Metab Res. 1992 Aug;24(8):367-70.
        • {MCE} [3]. Muindi JR et al. CYP24A1 inhibition enhances the antitumor activity of calcitriol. Endocrinology. 2010 Sep;151(9):4301-12.
        • {MCE} [4]. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161.
        • {MCE} [1]. Seif El-Din SH, et al. Effect of ketoconazole, a cytochrome P450 inhibitor, on the efficacy of quinine and halofantrine against Schistosoma mansoni in mice. Korean J Parasitol. 2013 Apr;51(2):165-75.
        • {MCE} [1]. Seif El-Din SH, et al. Effect of ketoconazole, a cytochrome P450 inhibitor, on the efficacy of quinine and halofantrine against Schistosoma mansoni in mice. Korean J Parasitol. 2013 Apr;51(2):165-75.
        • {MCE} [2]. Eil C. Ketoconazole binds to the human androgen receptor. Horm Metab Res. 1992 Aug;24(8):367-70.
        • {M
        • 65277-42-1 H98013 Ketoconazole
酮康唑

          化学属性

          Mol. FormulaC26H28Cl2N4O4
          Mol. Weight531
          TSCANo
          Melting Point148-152

          *以上化合物性质及应用等信息仅供参考