上海化源世纪贸易有限公司
上海市上海市普陀区
产品名：(2R,3R,4R,5R)-2-(((1S,2S,3R,4S,6R)-4-氨基-3-(((2S,3R)-3-氨基-6-(氨基甲基)-3,4-二氢-2H-吡喃-2-基)氧基)-6-(乙基氨基)-2-羟基环己基)氧基)-5-甲基-4-(甲基氨基)四氢-2H-吡喃-3,5-二醇硫酸盐(2:5)
纯度：98.0%
规格：
联系人：徐经理
联系电话：13311869306

上海吉至生化科技有限公司
上海市上海市奉贤区
产品名：硫酸奈替米星
纯度：98.0%
规格：50mg/100mg/10mg/5mg
联系人：刘佳
联系电话：18116092098

上海源溪生物科技有限公司
上海市上海市浦东新区
产品名：Netilmicin (sulfate)
纯度：98.9%
规格：1g
联系人：赖经理
联系电话：13564518121

上海脉铂医药科技有限公司
上海市上海市嘉定区
产品名：Netilmicin Sulfate
纯度：98.0%
规格：5mg/1g/1g/1g
联系人：李先生
联系电话：18916172912

上海创赛科技有限公司
上海市上海市嘉定区
产品名：[Perfemiker]奈替米星硫酸盐,≥98%
纯度：98.0%
规格：25mg/100mg/5mg
联系人：夏言
联系电话：18016376636

上海阿拉丁生化科技股份有限公司
上海市上海市浦东新区
产品名：奈替米星硫酸盐
纯度：98.0%
规格：100mg/25mg/1ml/1g
联系人：阿拉丁
联系电话：400-620-6333

湖北魏氏化学试剂股份有限公司
湖北省武汉市洪山区
产品名：硫酸奈替米星
纯度：98.0%
规格：5mg/25mg/10g/50g
联系人：张栋
联系电话：18717199209

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56391-57-2生产厂家

56391-57-2价格

56391-57-2

56391-57-2结构式

常用中文名：奈替米星硫酸盐
常用英文名：Netilmicin sulfate
CAS号：56391-57-2
分子式：C₂₁H₄₁N₅O_7.5/₂H₂O₄S
分子量：720.78
相关类别：原料药抗生素类药物氨基糖苷类药
发布时间：2018-02-04 08:00:00
更新时间：2024-01-04 18:58:34
Netilmicin硫酸盐是氨基糖苷类抗生素化合物。

化源商城直购

中文名	硫酸奈替米星
英文名	Netilmicin Sulfate
中文别名	1-N-乙基西索米星硫酸萘替米星USPEP 硫脲嘧啶
英文别名	certomycin EINECS 260-147-3 (1S,2S,3R,4S,6R)-4-Amino-3-{[(2S,3R)-3-amino-6-(aminomethyl)-3,4-dihydro-2H-pyran-2-yl]oxy}-6-(ethylamino)-2-hydroxycyclohexyl 3-deoxy-4-C-methyl-3-(methylamino)-β-L-arabinopyranoside sulfate (2:5) 1-N-Ethylsisomicin sulfate salt β-L-Arabinopyranoside, (1S,2S,3R,4S,6R)-4-amino-3-[[(2S,3R)-3-amino-6-(aminomethyl)-3,4-dihydro-2H-pyran-2-yl]oxy]-6-(ethylamino)-2-hydroxycyclohexyl 3-deoxy-4-C-methyl-3-(methylamino)-, sulfate (2 :5) (salt) Netilmicin sulfate Zetamicin MFCD01311715 Netillin Netilmicin sulfate salt UNII-S741ZJS97U Nettacin Netilmicin (sulfate)

描述	Netilmicin硫酸盐是氨基糖苷类抗生素化合物。
相关类别	信号通路 >> 抗感染 >> 细菌研究领域 >> 感染
参考文献	[1]. Campoli-Richards DM, et al. Netilmicin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1989 Nov;38(5):703-56. [2]. Adams E, et al. Determination of netilmicin sulfate by liquid chromatography with pulsed electrochemical detection. J Chromatogr A. 1998 Jul 3;812(1-2):151-7. [3]. Ciftci M, et al. Effects of some drugs on rat erythrocyte 6-phosphogluconate dehydrogenase: an in vitro and in vivo study. Pol J Pharmacol. 2002 May-Jun;54(3):275-80.

密度	1.32 g/cm3
沸点	684.3ºC at 760 mmHg
熔点	>194ºC (dec.)
分子式	C₂₁H₄₁N₅O_7.5/₂H₂O₄S
分子量	720.78
闪点	367.7ºC
PSA	814.36000
LogP	1.50400
外观性状	白色至灰白色粉末
储存条件	密封、在2 ºC -8 ºC下保存
稳定性	如果遵照规格使用和储存则不会分解，未有已知危险反应
水溶解性	H2O: soluble10mg/mL \| Soluble in water
计算化学	1、疏水参数计算参考值（XlogP）： 2、氢键供体数量：26 3、氢键受体数量：44 4、可旋转化学键数量：16 5、互变异构体数量： 6、拓扑分子极性表面积（TPSA）：773 7、重原子数量：91 8、表面电荷：0 9、复杂度：754 10、同位素原子数量：0 11、确定原子立构中心数量：22 12、不确定原子立构中心数量：0 13、确定化学键立构中心数量：0 14、不确定化学键立构中心数量：0 15、共价键单元数量：7
更多	1. 性状：白色至淡黄色粉末 2. 密度（g/mL,15ºC）：未确定 3. 相对蒸汽密度（g/mL,空气=1）：未确定 4. 熔点（ºC）：未确定 5. 沸点（ºC）：未确定 6. 沸点（ºC，14mmHg）：未确定 7. 折射率：未确定 8. 闪点（°C）：未确定 9. 比旋光度（ºC）：未确定 10. 自燃点或引燃温度（ºC）：未确定 11. 蒸气压（kPa,25ºC）：未确定 12. 饱和蒸气压（kPa,60ºC）：未确定 13. 燃烧热（KJ/mol）：未确定 14. 临界温度（ºC）：未确定 15. 临界压力（KPa）：未确定 16. 油水（辛醇/水）分配系数的对数值：未确定 17. 爆炸上限（%,V/V）：未确定 18. 爆炸下限（%,V/V）：未确定 19. 溶解性：极易溶于水，几乎不溶于乙醇及乙醚。

毒理学数据:

LD50(mg/kg)小鼠：静脉注射40，腹腔注射125，皮下注射175[1.19]

生态学数据:

对水是稍微有危害的不要让未稀释或大量的产品接触地下水、水道或者污水系统，若无政府许可，勿将材料排入周围环境。

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WK2286000

CAS REGISTRY NUMBER :: 56391-57-2

LAST UPDATED :: 199604

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C21-H41-N5-O7.5/2H2-O4-S

MOLECULAR WEIGHT :: 720.80

WISWESSER LINE NOTATION :: T6O BUTJ B1Z EZ FO- BL6TJ AZ CQ EM2 DO- BT6OTJ CQ DM1 EQ E1 ..H2.S-O4

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 :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,1249,1985

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 231 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 169 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 40700 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 167 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 189 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage)

REFERENCE :: AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 10,827,1976

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 68900 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 22 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 63100 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 420 mg/kg/14D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 375 mg/kg/30D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1365 mg/kg/26W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - interstitial nephritis Kidney, Ureter, Bladder - changes in bladder weight Blood - pigmented or nucleated red blood cells

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,499,1982 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 138 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,614,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 550 mg/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 :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,614,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 650 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,643,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 455 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,659,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4347 No. of Facilities: 25 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 2440 (estimated) No. of Female Employees: 1459 (estimated)

符号	GHS07, GHS08
信号词	Danger
危害声明	H312 + H332-H360
警示性声明	P201-P261-P280-P308 + P313
个人防护装备	Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
危害码 (欧洲)	T:Toxic;
风险声明 (欧洲)	R60;R20/21/22
安全声明 (欧洲)	S53-S36/37/39-S45
危险品运输编码	NONH for all modes of transport
WGK德国	3
RTECS号	WK2286000
海关编码	2942000000

参考文献[12~15]推荐如下路线和方法$

(1)3,2’,6’-三（N-乙酰）西索米星（023-2）的制备

在反应瓶中加入二甲基甲酰胺（DMF）/水的混合溶液100ml(DMF/水,体积比6:2)和乙酸铜5.5g(0.03mol),搅拌悬浮,再加入西索米星(023-1)4.5g(0.01mol),搅拌下加三乙胺调至PH8.5~10.5,在搅拌30min后降温至5 ºC 慢慢滴加乙酸酐3.1g(0.03mol)的3.5mlDMF溶液,滴加时控温在0~10 ºC ,在强烈搅拌下,并不断用三乙胺调节反应液的PH保持8.5~10.5,滴毕,室温(25 ºC)搅拌反应30min~1h.用TLC跟踪显示反应达终点后(如果未达到终点应补乙酸酐的DMF溶液适量),将反应液减压下浓缩,浓缩液用水稀释,冷至(0~10 ºC )保持4h.过滤去固体,滤液用阳离子交换树脂处理,氨水洗脱等处理后得023-2 5.2g,收率90%.

(2)5,2’’,4’’-三(三甲基硅)-3,2’,6’-三(N-乙酰)-西索米星(023-3)的制备

在反应瓶中加入023-2 10g(17.45mmol)、1,2-二甲氧基乙烷(DMF)100ml,搅拌溶解,再加入三甲基氯硅烷25ml(21.15g,194mmol),加热至50 ºC ,搅拌反应16h(在保持50~55 ºC 下)减压蒸除DME,得黄色固体023-3 13.5g,收率93.6%左右,含量91%.经硅胶柱色谱纯化可制得分析试样.

(3)5,2’’,4’’-三(三甲基硅)-1-乙基氨基-3,2’,6’-三(N-乙酰)西索米星(023-5)的制备

在反应瓶中加入化合物023-3 8g(9.5mmol)和水80ml,搅拌溶解,用4mol/L盐酸调至PH6.降温至15 ºC ,加入乙醛2.2ml(1.72g,39mmol),搅拌反应30min,生成亚胺化合物023-4溶液.将NaBH4的水溶液5ml[1g(26.47mmol)NaBH4溶于5ml水]匀速滴入上述含023-4的溶液，并用0.5mol/L盐酸严格控制PH6.继续反应30min,加入0.05mol/L硼砂溶液20ml(PH9.5)继续搅拌1h.得023-5的溶液,含量85%,备用.

(4)O-3-脱氧-4-C-甲基-3-(甲氨基)-B-L-阿拉伯吡喃糖苷(1—6)-O-[2,6-二氨基-2,3,4,6-四脱氧-a-D-甘油己糖-4-烯醇型吡喃糖苷基-(1—4)]-2-脱氧-N’-乙基-D-链霉胺硫酸盐(硫酸奈替米星)(023)的合成

在反应瓶中加入上步制备的含化合物023-5的溶液、珠粒状固体NaOH2g(50mmol)和Na2CO3 2.7g(25.5mmol),搅拌溶解,油浴加热升温至110 ºC ,在该温度下搅拌回流36h.降温至10~15 ºC,加入10mol/L H2SO4调反应液PH至6.5~7.0,抽滤,滤液即为奈替米星游离碱的澄清溶液,含量80%.

在上述澄清溶液中加入阳离子交换树脂,搅拌混合充分后,过滤,用7%氨水洗脱,洗脱液浓缩后用甲醇溶解,再上硅胶柱色谱分离纯化,用氯仿/甲醇/水(40:20:7)洗脱分离.将洗脱液减压浓缩至约10ml,加入活性炭0.5g,恒温水浴加热至50 ºC ,脱色30min.抽滤,滤液用10mol/L H2SO4调至PH3.5~5.5,匀速滴至无水乙醇300ml中,3h后抽滤,滤饼干燥,得023 5.93g,收率78.7,含量在97%以上,符合《中国药典》(2005年版)质量标准.该品为非结晶性固体(冷冻干燥).

海关编码	2942000000

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