9087-70-1 抑肽酶

抑肽酶

英文名称:Aprotinin
CAS:

9087-70-1

分子式:
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  • 化合物简介
  • 基本信息
  • 编号系统
  • 生产方法及用途

抑肽酶简介

The drug aprotinin (Trasylol, previously Bayer and now Nordic Group pharmaceuticals), is the small protein bovine pancreatic trypsin inhibitor (BPTI), an antifibrinolytic molecule that inhibits trypsin and related proteolytic enzymes. Under the trade name Trasylol, aprotinin was used as a medication administered by injection to reduce bleeding during complex surgery, such as heart and liver surgery. Its main effect is the slowing down of fibrinolysis, the process that leads to the breakdown of blood clots. The aim in its use was to decrease the need for blood transfusions during surgery, as well as end-organ damage due to hypotension (low blood pressure) as a result of marked blood loss. The drug was temporarily withdrawn worldwide in 2007 after studies suggested that its use increased the risk of complications or death; this was confirmed by follow-up studies. Trasylol sales were suspended in May 2008, except for very restricted research use. In February 2012 the European Medicines Agency (EMA) scientific committee reverted its previous standpoint regarding aprotinin, and has recommended that the suspension be lifted. Nordic became distributor of aprotinin in 2012.

抑肽酶基本信息

中文名称 抑肽酶 英文名称 Aprotinin
中文别名

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英文别名

cas9004-04-0; Trypsin Inhibitor;

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CAS号 9087-70-1 分子式
分子量 0.00000 精确质量 0.00000
PSA 0.00000 LOGP 0.00000

抑肽酶编号系统

UNII 04XPW8C0FL

生产方法及用途

生产方法

抑肽酶可以从牛胰和肺组织中提取,也可以从人尿中提取。目前国内主要从牛肺中提取。 取新鲜牛肺冲洗干净,用绞肉机绞碎。然后加入5倍体积的水,搅拌均匀,用2.5mol/L的硫酸调节pH=2.0,搅拌提取8h,然后用双层纱布过滤,滤渣重复上述步骤再提取一次,合并两次提取液。向提取液中按每升277g加入硫酸铵,搅匀,再用5mol/L的硫酸调节pH=1.5,静置过夜。吸取上清液,过滤,滤液调节pH=5.5,再按每升加255g向滤液中加入硫酸铵,搅匀,静置48h,过滤,收集盐析物。盐析物用8~10倍水溶解,4℃下静置过夜,滤去沉淀,滤液中加入50%三氯乙酸(加量为滤液的1/20),搅匀,迅速加热至80℃后速冷到30℃,滤去沉淀,再用20%的氢氧化钠调pH=3.0,然后加入硫酸铵(每升滤液加610g),搅拌溶解,静置过夜,收集盐析物。盐析物再用5倍的
0 1mol/L乙酸钠(pH=5
.5)缓冲液和1倍体积的硼酸缓冲液溶解,再加入硫酸镁(每升加1050g),搅拌溶解,静置过夜,收集沉淀,弃滤液。沉淀用4倍体积的水溶解后,透析24h,加硅藻土过滤,滤液用201×7和001×7型树脂吸附(二者比例为3
∶1),过滤树脂,得脱盐液。脱盐液中加0.9%氯化钠和1.5倍丙酮,析出沉淀,过滤。沉淀用丙酮和乙醚洗涤,干燥,然后再溶于60倍量80%甲醇中,过滤。滤液中再加入适量的氯化钠和丙酮,搅匀,静置过夜,离心,沉淀用丙酮洗涤后,干燥,可得沉淀物。沉淀物用无热源的水溶解,调节pH=11,4℃下放置过夜,过滤,滤液用乙酸调节pH=4~5,再加入1%氯化钠溶液(浓度30%)及5倍量丙酮,静置过夜,收集沉淀,并用丙酮和乙醚洗涤,干燥,可得成品。

用途

1.对胰蛋白酶、糜蛋白酶、凝白酶、溶血纤维蛋白酶以及各种组织或血浆激肽释放酶有广谱抑制作用。可用于治疗急性胰腺炎,并对皮肤疾患、烧伤休克及产后大出血有独特的疗效。

抑肽酶
CAS号:9087-70-1 分子式: 分子量:0.00000

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