107667-60-7

• 常用中文名：L-肌肽锌
• 常用英文名：Polaprezinc
• CAS号：107667-60-7
• 分子式：C₉H₁₁N₄O₃Zn
• 分子量：288.59
• 相关类别： 研究领域 炎症/免疫
• 发布时间：2018-03-27 08:00:00
• 更新时间：2024-01-02 23:10:24
• Polaprezinc 是由锌、L-肌肽构成的口服螯合物,具有抗氧化、抗溃疡、抗炎活性。

名称

• 中文名: 聚普瑞锌
• 英文名: Polaprezinc
• 中文别名: 肌肽锌; L-肌肽锌
• 英文别名: Zinc L-carnosine; Zinc Carnosine; Zinc, [β-​alanyl-​κN-​L-​histidinato(2-​)​-​κN,​κO]​- (9CI); MFCD00870906; Histidine, β-alanyl-, zinc salt (1:1); Zinc 2-(β-alanylamino)-3-(imidazol-3-id-4-yl)propanoate

物化性质

• 沸点: 557.6ºC at 760 mmHg
• 熔点: 300ºC
• 分子式: C₉H₁₁N₄O₃Zn
• 分子量: 288.59
• 闪点: 291ºC
• PSA: 101.31000
• 外观性状: 白色结晶
• 储存条件: Refrigerator

生物活性

• 描述: Polaprezinc 是由锌、L-肌肽构成的口服螯合物,具有抗氧化、抗溃疡、抗炎活性。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 炎症/免疫
• 体内研究: Polaprezinc(PZ)是一种抗溃疡药物和螯合化合物,由锌离子,L-肌肽,β-丙氨酸二肽和L-组氨酸组成。 Polaprezinc具有抗氧化作用,可清除自由基。据报道Polaprezinc在动物模型中对急性放射性直肠炎有效,并证明Polaprezinc在暴露于放射线后具有抗炎作用[1]。
• 动物实验: 小鼠[1]使用雄性C57BL / 6J小鼠（8周龄;体重，~20g）。使小鼠适应7天。它们被安置在4-5个/笼中，并随意喂养实验室啮齿动物颗粒配方和自来水。将小鼠维持在22℃±0.5℃的恒定温度，50％±5％的湿度下并暴露于12小时光/暗循环。小鼠口服在饮用水中接受100mg / kg体重的Polaprezinc。使用150kVp的X射线单元以~200cGy / min的剂量率照射小鼠。对于剂量测定，连接到静电计系统的探针靠近目标位置放置。
• 参考文献:

  [1]. Odawara S, et al. Polaprezinc protects normal intestinal epithelium against exposure to ionizing radiation in mice. Mol Clin Oncol. 2016 Oct;5(4):377-381.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : ZQ8800000 CHEMICAL NAME : Zinc, (N-beta-alanyl-L-histidinato(2-)-N,N(sup N),O(sup alpha))- CAS REGISTRY NUMBER : 107667-60-7 LAST UPDATED : 199801 DATA ITEMS CITED : 14 MOLECULAR FORMULA : C9-H12-N4-O3-Zn MOLECULAR WEIGHT : 289.62 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 : 7375 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1033,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 405 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1033,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1033,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1269 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1033,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 165 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1033,1991 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 758 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1033,1991 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >200 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 45,52,1995 TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Primate - monkey DOSE/DURATION : >626 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 43,562,1993 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 27 gm/kg/13W-I TOXIC EFFECTS : Endocrine - changes in adrenal weight Blood - pigmented or nucleated red blood cells Blood - other changes REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1036,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 54600 mg/kg/52W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes in urine composition Blood - pigmented or nucleated red blood cells Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1036,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 27 gm/kg/13W-I TOXIC EFFECTS : Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 45,52,1995 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 18200 mg/kg/13W-I TOXIC EFFECTS : Liver - other changes Kidney, Ureter, Bladder - other changes Nutritional and Gross Metabolic - changes in metals, not otherwise specified REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 43,562,1993 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 10250 mg/kg SEX/DURATION : female 17-21 day(s) after conception lactating female 20 day(s) post-birth TOXIC EFFECTS : Reproductive - Maternal Effects - parturition REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1042,1991 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 3900 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 41,1042,1991

合成路线

1535206-09-7 ~% 107667-60-7

文献：Angewandte Chemie - International Edition, , vol. 53, # 1 p. 193 - 198 Angew. Chem., , vol. 126, # 1 p. 197 - 202,6

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