Mometasone Furoate 糠酸莫美他松

CAS 83919-23-7 MFCD00866003

化学结构图

83919-23-7
SMILES: C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(Cl)[C@@H](O)C[C@]2(C)[C@@]1(OC(=O)c1ccco1)C(=O)CCl

化学属性

Mol. FormulaC27H30Cl2O6
Mol. Weight521
Melting Point212-216
Appearance Solid powder
SolubilitySoluble in DMSO.

别名和识别编码

Chemical NameMometasone Furoate
Synonym (11,16)-9,21-Dichloro-17-[(2-furanylcarbonyl)oxy]-11-hydroxy-16-methylpregna-1,4-diene-3,20-dione (11β,16α)-9,21-Dichloro-17-[(2-furanylcarbonyl)oxy]-11-hydroxy-16-methylpregna-1,4-diene-3,20-dione ELOCON brand of mometasone furoate cream (0.1)
MDL NumberMFCD00866003
CAS Number83919-23-7
Chemical Name Translation糠酸莫美他松
Reaxys-RN4340538
PubChem Substance ID172088987
Merck Number6241
Beilstein Registry Number4340538
FormulaC27H30Cl2O6
IUPAC Name(8S,9R,10S,11S,13S,14S,16R,17R)-9-chloro-17-(2-chloroacetyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl furan-2-carboxylate
InChIKeyWOFMFGQZHJDGCX-ZULDAHANSA-N
InChIInChI=1S/C27H30Cl2O6/c1-15-11-19-18-7-6-16-12-17(30)8-9-24(16,2)26(18,29)21(31)13-25(19,3)27(15,22(32)14-28)35-23(33)20-5-4-10-34-20/h4-5,8-10,12,15,18-19,21,31H,6-7,11,13-14H2,1-3H3/t15-,18+,19+,21+,24+,25+,26+,27+/m1/s1
Canonical SMILESO=C(C1=CC=CO1)O[C@]2(C(CCl)=O)[C@H](C)C[C@@]3([H])[C@]4([H])CCC5=CC(C=C[C@]5(C)[C@@]4(Cl)[C@@H](O)C[C@]23C)=O
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分类

  • {SNA} Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Cytokines, Growth Factors and Hormones, Fluorination Ready Pharma-Developed Compounds, Hormones, M, Other Steroid Products, Schering Plough, Steroid Hormones, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学
  • Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Cytokines, Growth Factors and Hormones, Hormones, Other Steroid Products, Schering Plough, Steroid Hormones

产品应用

  • Like other topical corticosteroids, mometasone furoate has anti-inflammatory, antipruritic, and vasoconstrictive properties. The mechanism of the anti- inflammatory activity of the topical steroids, in general, is unclear. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. The extent of percutaneous absorption of topical corticosteroids is determined by many factors including the vehicle and the integrity of the epidermal barrier. (Source: http://www.rxlist.com/elocon-drug.htm)

相关文献及参考

  • [2]. https://go.drugbank.com/drugs/DB14512
  • Derendorf, H., and Meltzer, E.O., Molecular and clinical pharmacology of intranasal corticosteroids: clinical and therapeutic implications. Allergy 63 , 1292-1300, (2008)
  • Merck 14 ,6241
  • Ogawa, M., et al., Dissociation of local anti-inflammatory effect and systemic effects of mometasone furoate in mice. Immunopharmacol. Immunotoxicol. 31 , 601-606, (2009) 摘要
  • Sivam, A., et al., Olfactory cleft inflammation is present in seasonal allergic rhinitis and is reduced with intranasal steroids. Am. J. Rhinol. Allergy 24 , 286-290, (2010) 摘要
  • [1]. Maria Galuppo, et al. Use of Mometasone furoate in prolonged treatment of experimental spinal cord injury in mice: A comparative study of three
  • [1]. Maria Galuppo, et al. Use of Mometasone furoate in prolonged treatment of experimental spinal cord injury in mice: A comparative study of three different glucocorticoids. Pharmacol Res. 2015 Sep;99:316-28

安全信息

WGK Germany3
RTECSTU3822000
Storage condition 0-10 0-10°C Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Signal word
Hazard statements
  • H361 Suspected of damaging fertility or the unborn child 怀疑对生育能力或未出生婴儿造成伤害
Precautionary statements
  • P201 Obtain special instructions before use. 使用前获取专门指示。
  • P202 Do not handle until all safety precautions have been read and understood. 已阅读并理解所有的安全预防措施之前，切勿操作。
  • P262 Do not get in eyes, on skin, or on clothing. 不要接触眼睛，皮肤或衣服。
  • P280 Wear protective gloves/protective clothing/eye protection/face protection. 戴防护手套/防护服/眼睛的保护物/面部保护物。
  • P281 Use personal protective equipment as required. 使用所需的个人防护装备。
  • P308+P313
  • P405 Store locked up. 上锁保管。
  • P501 Dispose of contents/container to..… 处理内容物/容器.....
GHS Symbol 
TYPE OF TEST            : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 1 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
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: 24,4203,1990

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 300 mg/kg
TOXIC EFFECTS :
   Lungs, Thorax, or Respiration - respiratory depression
   Nutritional and Gross Metabolic - body temperature decrease
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: 24,4203,1990

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 330 ug/kg
SEX/DURATION            : female 7-17 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight
   gain)
   Reproductive - Effects on Newborn - physical
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: 24,2517,1990

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 66 ug/kg
SEX/DURATION            : female 7-17 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
   e.g., stunted fetus)
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 24,2517,1990

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
D

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Administration onto the skin
SPECIES OBSERVED        : Rodent - rabbit
DOSE                    : 2600 ug/kg
SEX/DURATION            : female 6-18 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 24,2545,1990

系列性分类

  1. Life Science 生命科学
  2. Cell Biology 细胞生物学
  3. Cell Signaling and Neuroscience - Cell Biology
  4. Cytokines, Growth Factors and Hormones - Cell Signaling and Neuroscience
  5. Hormones - Cytokines, Growth Factors and Hormones
  6. Steroid Hormones - Hormones
  7. Other Steroid Products - Steroid Hormones
  1. Medical Research Areas
  2. Metabolism
  3. Phospholipase (e.g. PLA)
  1. Medical Research Areas
  2. GPCR & G Protein
  3. Glucocorticoid Receptor  (糖皮质激素受体)

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