阿氯米松双丙酸酯
阿氯米松双丙酸酯用途
二丙酸氯米松(Sch 22219)是一种类固醇化合物。二丙酸氯米松可用于皮炎和皮肤瘙痒的研究[1][2]。
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阿氯米松双丙酸酯名称
[ CAS 号 ]:
66734-13-2
[ 中文名 ]:
阿氯米松双丙酸酯
[ 英文名 ]:
Aclovate
[中文别名 ]:
[英文别名 ]:
- alclometasone Dipropionate
- Modrasone
- alclovate
- Delonal
- Almeta
- Alclometasone-17,21-dipropionate
- Ddlonal
- ALCLOMETASONEDIPROPIONATE,USP
- Aclovate
- Vitra
阿氯米松双丙酸酯生物活性
[ 描述 ]:
二丙酸氯米松(Sch 22219)是一种类固醇化合物。二丙酸氯米松可用于皮炎和皮肤瘙痒的研究[1][2]。
[ 相关类别 ]:
[体外研究]
丙酸阿氯米松(0.01-100 ng/mL；24 h)抑制人PBMC中CD3/CD2刺激的细胞因子产生,IL-2、IL-3、IL-4、IL-5、IFN-γ和GM-CSF的IC50分别为5.54、1.76、2.09、0.89、3.26和0.76 ng/mL[1]。
[体内研究]
二丙酸氯米松(0.1%(20μL)；耳朵两侧；一次)显示出对结核菌素和卵清蛋白诱导的过敏反应的影响[2]。动物模型：结核菌素诱导迟发性过敏反应的Lewis大鼠[2]剂量：0.1%(20μL)给药：双侧耳；0.1%(20μ。动物模型：具有卵清蛋白诱导的被动皮肤过敏反应的棕色挪威大鼠[2]剂量：0.1%(20μL)给药：耳朵两侧；0.1%(20μL)卵蛋白激发前6小时结果：显著抑制了这种被动皮肤过敏反应中染料泄漏量的增加。
阿氯米松双丙酸酯物理化学性质
[ 密度 ]:
1.26g/cm3
[ 沸点 ]:
636ºC at 760 mmHg
[ 分子式 ]:
C28H37ClO7
[ 分子量 ]:
521.04200
[ 闪点 ]:
338.4ºC
[ 精确质量 ]:
520.22300
[ PSA ]:
106.97000
[ LogP ]:
3.94270
[ 折射率 ]:
1.562
[ 储存条件 ]:
库房通风低温干燥,与食品原料分开存放
阿氯米松双丙酸酯毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- TU3790000
- CHEMICAL NAME :
- Pregna-1,4-diene-3,20-dione, 7-chloro-11-hydroxy-16-methyl-17,21-bis(1-oxopropoxy) -, (7-alpha,11-beta,16-alpha)-
- CAS REGISTRY NUMBER :
- 66734-13-2
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 17
- MOLECULAR FORMULA :
- C28-H37-Cl-O7
- MOLECULAR WEIGHT :
- 521.10
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 3593 mg/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: -,70,1990
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >75 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- 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: 19,735,1988
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 3593 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Skin and Appendages - hair
- 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: 21,1253,1987
- 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). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,70,1990
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 2506 mg/kg
- TOXIC EFFECTS :
- Behavioral - somnolence (general depressed activity) Skin and Appendages - hair
- 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: 21,1253,1987
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >15 mg/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: -,70,1990
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >15 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- 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: 19,735,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 9 mg/kg/90D-I
- TOXIC EFFECTS :
- Blood - changes in leukocyte (WBC) count Blood - changes in platelet count Nutritional and Gross Metabolic - weight loss or decreased weight gain
- 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: 21,1351,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 18250 ug/kg/1Y-I
- TOXIC EFFECTS :
- Blood - pigmented or nucleated red blood cells Blood - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain
- 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: 21,1437,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 9 mg/kg/90D-I
- TOXIC EFFECTS :
- Endocrine - changes in spleen weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
- 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: 21,1309,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 18 mg/kg/90D-C
- TOXIC EFFECTS :
- Liver - other changes Endocrine - adrenal cortex hypoplasia Blood - other changes
- 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: 21,1389,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 36500 ug/kg/1Y-I
- TOXIC EFFECTS :
- Endocrine - changes in adrenal weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain
- 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: 21,1483,1987 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 11 mg/kg
- SEX/DURATION :
- female 7-17 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,301,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- DOSE :
- 1100 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)
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,301,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- DOSE :
- 18 mg/kg
- SEX/DURATION :
- male 90 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands
- 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: 21,1389,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- DOSE :
- 18 mg/kg
- SEX/DURATION :
- female 90 day(s) pre-mating
- TOXIC EFFECTS :
- Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - uterus, cervix, vagina
- 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: 21,1389,1987
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Administration onto the skin
- DOSE :
- 1300 ug/kg
- SEX/DURATION :
- female 6-18 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth)
- REFERENCE :
- OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 33,343,1987
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阿氯米松双丙酸酯安全信息
[ 符号 ]:
GHS08
[ 信号词 ]:
Warning
[ 危害声明 ]:
H361d
[ 警示性声明 ]:
P280
[ 危险品运输编码 ]:
NONH for all modes of transport
阿氯米松双丙酸酯合成路线
阿氯米松双丙酸酯上下游产品
阿氯米松双丙酸酯上游产品
阿氯米松双丙酸酯下游产品
阿氯米松双丙酸酯制备
化合物(Ⅰ)在2，3-二氯-5，6-二氰基苯醌(DDQ)作用下，脱去一分子氢，在6、7位形成双键，而得化合物(Ⅱ)。碳酸氢钠水解21位的酯后，和原丙酸三乙酯反应，使17位和21位的羟基形成环状原甲酸酯(Ⅳ)。在醋酸中重排成17位丙酸酯(V)。然后和丙酸酐反应，使21位羟基成丙酸酯，而得到双丙酸酯(Ⅵ)。最后和氯化氢加成，得到双丙酸阿氯米松。总收率2.678%。
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相关化工产品/化学物质：
推荐生产厂家/供应商：
公司名：上海源溪生物科技有限公司
区域：上海市浦东新区
价格：
￥需询单/1g
联系人：赖经理
产品详情：Aclovate
公司名：上海脉铂医药科技有限公司
区域：上海市嘉定区
价格：
￥2576.0/25mg
￥1213.0/10mg
￥716.0/5mg
￥需询单/1g
联系人：李先生
产品详情：Alclometasone Dipropionate
公司名：上海阿拉丁生化科技股份有限公司
区域：上海市浦东新区
价格：
￥3385.0/25mg
￥需询单/1g
￥需询单/1g
￥需询单/1g
联系人：阿拉丁李高志
产品详情：丙酸氯米松
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