98753-19-6

• 常用中文名：硫酸头孢匹罗
• 常用英文名：Cefpirome sulfate
• CAS号：98753-19-6
• 分子式：C₂₂H₂₄N₆O₉S₃
• 分子量：612.656
• 相关类别： 原料药 抗生素类药物 头孢菌素类药
• 发布时间：2018-08-20 15:03:51
• 更新时间：2024-01-02 15:39:42
• Cefpirome sulfate (HR-810 sulfate) 是第四代头孢类抗生素, 具广谱抗菌活性, 对葡萄球菌、耐青霉素的肺炎球菌及肠球菌均有效。
• 硫酸头孢匹罗是由德国赫司特公司和法国Roussel公司共同研制开发的第四代头孢菌素，是近年来开始应用于国外临床的新一代头孢菌素，与第一、二、三代头孢菌 素相比，第四代头孢菌素抗菌谱更广、对β-内酰胺酶更稳定、血药浓度高、可透过血脑屏障等优点。头孢匹罗为第四代头孢菌素中的优秀新品种，本品具有抗菌作 用强，抗菌谱广，对革兰氏阳性菌（如葡萄球菌属、粪肠球菌）、革兰氏阴性菌（如布兰氏球菌属、假单胞菌）及厌氧菌具有广泛的抗菌谱和较强的杀菌作用。对 β-内酰胺酶稳定性高，能很好地向痰液、胆液、腹腔内、创伤渗出液、女性性器官、前列腺和脑脊液中转移。临床上证实了对败血症和外伤、手术创伤等浅表的二 次感染有很好的疗效。头孢匹罗对细菌性脑膜炎致病菌有很好的杀菌活性，对血脑屏障有良好的穿透性，故本品在治疗脑膜炎感染中取得良好疗效。虽然头孢匹罗 半衰期较短（约2h），但药物在体液中的浓度高，可以适当减少头孢喹咪的用量，使既达到满意的抗菌效果，又能减少治疗费用。目前头孢匹罗已经成功地用于医 院和社区获得性严重下呼吸道感染；白细胞减少病人的感染；重症监护病人的严重感染；败血症/菌血症；皮肤和软组织感染；复杂性上、下尿道感染；脑膜炎等的 治疗。

名称

• 中文名: 硫酸头孢匹罗
• 英文名: Cefpirome Sulfate
• 中文别名: 硫酸头孢匹罗; 1-[7-(2-氨基-4-噻唑基)-2-(甲氧亚氨基)乙酰氨基]-2-羧基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-3-基]甲基-6,7-二氢-5H-环戊二烯并吡啶鎓硫酸盐
• 英文别名: Cefpirome sulfate; HR 810 sulfate; (6R,7R)-7-{[(2Z)-2-(2-Amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-(6,7-dihydro-5H-cyclopenta[b]pyridinium-1-ylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate sulfate; MFCD01688770; (6R,7R)-7-{[(2Z)-2-(2-Amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-(6,7-dihydro-5H-cyclopenta[b]pyridinium-1-ylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-2-carboxylatsulfat; (6R,7R)-7-{[(2Z)-2-(2-Amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino}-3-(6,7-dihydro-5H-cyclopenta[b]pyridinium-1-ylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate sulfate (1:1); cefpirome sulphate; CefpiromeSulfate; Cefpirome (sulfate)

物化性质

• 熔点: 198-202ºC
• 分子式: C₂₂H₂₄N₆O₉S₃
• 分子量: 612.656
• 精确质量: 612.076660
• PSA: 290.44000
• LogP: 0.29410
• 外观性状: 白色或灰白色结晶粉末
• 储存条件: Store at 0-5°C
• 水溶解性: 水溶性：可溶；不溶：乙醚,乙醇

生物活性

• 描述: Cefpirome sulfate (HR-810 sulfate) 是第四代头孢类抗生素, 具广谱抗菌活性, 对葡萄球菌、耐青霉素的肺炎球菌及肠球菌均有效。
• 相关类别:
  信号通路 >> 抗感染 >> 细菌
  研究领域 >> 感染

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UW8970000 CAS REGISTRY NUMBER : 98753-19-6 LAST UPDATED : 199512 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C22-H23-N6-O5-S2.H-O4-S MOLECULAR WEIGHT : 612.70 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 : >8 gm/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),1,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 5800 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),1,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >10 gm/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),1,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1900 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),1,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 16200 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),1,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 3850 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),1,1990 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 2400 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),1,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 36 gm/kg/90D-I TOXIC EFFECTS : Kidney, Ureter, Bladder - changes in bladder weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in erythrocyte (RBC) count REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 40,1034,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 45 gm/kg/90D-I TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 40,1250,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 75200 mg/kg/26W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - changes in bladder weight Blood - changes in erythrocyte (RBC) count REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 40,1250,1990 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 8800 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - physical REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),65,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 20800 mg/kg SEX/DURATION : female 17-21 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),91,1990 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous DOSE : 8800 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15(Suppl 3),65,1990

合成路线

84957-29-9 ~% 98753-19-6

文献：Duan, Xuemin; Lu, Yao; Han, Juan; Chen, Ligong; Zheng, Pengwu Synthetic Communications, 2011 , vol. 41, # 5 p. 629 - 636

1273319-61-1 ~% 98753-19-6

文献：Synthetic Communications, , vol. 41, # 5 p. 629 - 636

95055-53-1 ~% 98753-19-6

文献：Synthetic Communications, , vol. 41, # 5 p. 629 - 636

104146-10-3 ~% 98753-19-6

文献：Synthetic Communications, , vol. 41, # 5 p. 629 - 636

101156-40-5 ~% 98753-19-6

文献：Synthetic Communications, , vol. 41, # 5 p. 629 - 636

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