72324-18-6

• 常用中文名：司替罗宁
• 常用英文名：Stepronin
• CAS号：72324-18-6
• 分子式：C₁₀H₁₁NO₄S₂
• 分子量：273.32900
• 相关类别： 研究领域 内分泌
• 发布时间：2018-07-25 12:31:37
• 更新时间：2024-01-02 13:39:07
• Stepronin(前列甘氨酸)是一种口服活性祛痰剂(吸入给药优于口服给药)。Stepronin通过减少上皮细胞的Cl-分泌和粘膜下腺的粘液糖蛋白分泌来抑制体外气道分泌[1]。

名称

• 中文名: 司替罗宁
• 英文名: 2-[2-(thiophene-2-carbonylsulfanyl)propanoylamino]acetic acid
• 中文别名: 2-[(2-噻吩甲酰基硫)丙酰胺基]乙酸
• 英文别名: Stepronine; Steproninum; Prostenoglycine; Bronco-plus; MFCD00867405; EINECS 276-587-4; Stepronin; Tiofacic; Tiase; Stepronino

物化性质

• 密度: 1.428 g/cm3
• 沸点: 521.2ºC at 760 mmHg
• 熔点: 168-170ºC
• 分子式: C₁₀H₁₁NO₄S₂
• 分子量: 273.32900
• 闪点: 269ºC
• 精确质量: 273.01300
• PSA: 137.01000
• LogP: 1.60170
• 外观性状: 白色或灰白色结晶
• 折射率: 1.609

生物活性

• 描述: Stepronin(前列甘氨酸)是一种口服活性祛痰剂(吸入给药优于口服给药)。Stepronin通过减少上皮细胞的Cl-分泌和粘膜下腺的粘液糖蛋白分泌来抑制体外气道分泌[1]。
• 相关类别:
  研究领域 >> 内分泌
  信号通路 >> 其他 >> 其他
• 体外研究: Stepronin(0.1-100µM；20分钟)以剂量依赖性方式诱导犬气管上皮中ISOP(异丙肾上腺素)诱发的SCC(短路电流)值显著降低[1]。Stepronin(10-100µM；20分钟)以剂量依赖性方式显著抑制犬气管上皮细胞的基础分泌和ISOP诱发的PD(电位差)值[1]。Stepronin(100µM；20分钟)显著抑制ISOP诱导的粘膜下腺体[3H]-糖缀合物分泌[1]。细胞活力测定[1]细胞系：犬气管上皮(来自成年和10至25 kg体重的男女杂种狗)浓度：0.1-100µM；10-100µM培养时间：20分钟(治疗前)结果：显著抑制ISOP诱导的SCC和PD值以及基础分泌。细胞活力测定[1]细胞系：粘膜下腺(来自成年和10至25 kg体重的男女杂种狗)浓度：100µM培养时间：20分钟(治疗前)结果：显著抑制ISOP诱导的[3H]-糖缀合物分泌。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : MC0813680 CHEMICAL NAME : Glycine, N-(1-oxo-2-((2-thienylcarbonyl)thio)propyl)- CAS REGISTRY NUMBER : 72324-18-6 LAST UPDATED : 199201 DATA ITEMS CITED : 8 MOLECULAR FORMULA : C10-H11-N-O4-S2 MOLECULAR WEIGHT : 273.34 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 : >2500 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4242354 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1140 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 20,310,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1801 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4242354 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 3336 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 20,310,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1511 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 20,310,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >1250 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4242354 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 1584 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 20,310,1984 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 534 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 20,310,1984