65089-17-0

• 常用中文名：匹立昔尔
• 常用英文名：Pirinixil
• CAS号：65089-17-0
• 分子式：C₁₆H₁₉ClN₄O₂S
• 分子量：366.86600
• 相关类别： 研究领域 代谢疾病
• 发布时间：2018-06-22 01:36:06
• 更新时间：2024-01-02 14:44:54
• Pirinixil 是一种低毒性降血脂药。

名称

• 中文名: 匹立昔尔
• 英文名: 2-[4-chloro-6-(2,3-dimethylanilino)pyrimidin-2-yl]sulfanyl-N-(2-hydroxyethyl)acetamide
• 英文别名: 2-[4-chloro-6-(2,3-dimethyl-anilino)-pyrimidin-2-ylsulfanyl]-N-(2-hydroxy-ethyl)-acetamide; Pirinixil; BR-931; <<4-chloro-6-<(2,3-dimethylphenyl)amino>-2-pyrimidinyl>thio>-N-(2-hydroxyethyl)acetamide; 2-((4-Chloro-6-((2,3-dimethylphenyl)amino)-2-pyrimidinyl)thio)-N-(2-hydroxyethyl)acetamide; Pirinixilo [Spanish]; Pirinixilum [INN-Latin]; Pirinixilo [INN-Spanish]

物化性质

• 密度: 1.37g/cm3
• 沸点: 609.6ºC at 760 mmHg
• 分子式: C₁₆H₁₉ClN₄O₂S
• 分子量: 366.86600
• 闪点: 322.5ºC
• 精确质量: 366.09200
• PSA: 112.44000
• LogP: 3.15490
• 折射率: 1.642
• 储存条件: 2-8℃

生物活性

• 描述: Pirinixil 是一种低毒性降血脂药。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 代谢疾病
• 体内研究: Pirinixil是一种低毒的降血脂药。 Pirinixi在大鼠的脾脏,肾脏和心脏中降低总胆固醇。 Pirinixil使估计的总体内胆固醇降低约40％[1]。 Pirinixil可显着提高血浆胆固醇水平,而不会影响血浆甘油三酯。 Pirinixil显着降低肝脏胆固醇和甘油三酯,而血浆和肝脏脂质水平降低约20％。肝脏HMG-CoA还原酶活性不受影响,但Pirinixil可显着降低胆固醇7α-羟化酶[2]。
• 动物实验: 在所有研究中使用在每个实验开始时重220-230g的雄性Sprague-Dawley大鼠。它们被保存在空调环境中，拥有可控的照明和免费供水。膳食治疗是（A）大鼠的标准饮食和（B）2％胆固醇+ 2％胆酸方案。两种饮食分别随意给药1周和2周（标准饮食）和2周（胆固醇酸饮食）。在3个实验的每一个中的5只大鼠组（标准饮食1周和2周，胆固醇 - 胆酸饮食2周）通过胃插管每天在羧甲基纤维素载体中以20mg / kg的剂量施用Pirinixil。通过插管[1]每天给予对照相似体积的载体。
• 参考文献:

  [1]. D'Atri G, et al. Clofibrate, pirinixil (BR 931) and WY-14,643 do not affect body cholesterol in Sprague-Dawley rats. Atherosclerosis. 1980 Nov;37(3):475-83.

  [2]. Kritchevsky D, et al. Increased plasma cholesterol and decreased body lipid levels in Wistar rats following pirinixil(BR 931) treatment. Pharmacol Res Commun. 1979 Jun;11(6):475-82.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : AB5860000 CHEMICAL NAME : Acetamide, 2-((4-chloro-6-(2,3-xylidino)-2-pyrimidinyl)thio)-N-( 2-hydroxyethyl)- CAS REGISTRY NUMBER : 65089-17-0 BEILSTEIN REFERENCE NO. : 0845588 LAST UPDATED : 199612 DATA ITEMS CITED : 7 MOLECULAR FORMULA : C16-H19-Cl-N4-O2-S MOLECULAR WEIGHT : 366.90 WISWESSER LINE NOTATION : T6M CN BHJ BS1VM2Q DG FMR B1 C1 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 : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >5 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1575 mg/kg/21D-C TOXIC EFFECTS : Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - catalases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 17 gm/kg/81W-C TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other transferases TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 137 gm/kg/81W-C TOXIC EFFECTS : Tumorigenic - Carcinogenic by RTECS criteria Liver - tumors MUTATION DATA TYPE OF TEST : DNA inhibition TEST SYSTEM : Rodent - mouse Cells - not otherwise specified DOSE/DURATION : 25 umol/L REFERENCE : CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 40,36,1980

合成路线

17619-22-6 50892-23-4 ~% 65089-17-0

文献：L'Instituto Farmaceutico S.p.A. Patent: US4188484 A1, 1980 ;

541-41-3 141-43-5 50892-23-4 ~% 65089-17-0

文献：L'Instituto Farmaceutico S.p.A. Patent: US4188484 A1, 1980 ;

151-56-4 50892-23-4 ~56% 65089-17-0

文献：d'Atri; Gomarasca; Resnati; Tronconi; Scolastico; Sirtori Journal of Medicinal Chemistry, 1984 , vol. 27, # 12 p. 1621 - 1629

50892-49-4 ~% 65089-17-0

文献：d'Atri; Gomarasca; Resnati; Tronconi; Scolastico; Sirtori Journal of Medicinal Chemistry, 1984 , vol. 27, # 12 p. 1621 - 1629

91759-33-0 ~% 65089-17-0

文献：d'Atri; Gomarasca; Resnati; Tronconi; Scolastico; Sirtori Journal of Medicinal Chemistry, 1984 , vol. 27, # 12 p. 1621 - 1629

50892-12-1 ~% 65089-17-0

文献：d'Atri; Gomarasca; Resnati; Tronconi; Scolastico; Sirtori Journal of Medicinal Chemistry, 1984 , vol. 27, # 12 p. 1621 - 1629

65089-38-5 ~% 65089-17-0

文献：L'Instituto Farmaceutico S.p.A. Patent: US4188484 A1, 1980 ;

上下游产品

上游产品  7
17619-22-6 50892-23-4 541-41-3 141-43-5
151-56-4 50892-49-4 50892-12-1
下游产品  0