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分类

• Pharmaceuticals
• {SNA} Application Index, Approved Therapeutics/Drug Candidates, Bioactive Small Molecules,
• {SNA} Application Index, Approved Therapeutics/Drug Candidates, Bioactive Small Molecules, Biochemicals and Reagents, Cell Signaling Enzymes, Cell Signaling and Neuroscience, Drug Efflux Pumps, Drug Transport Compounds, Drug Transport Proteins & Reagents, Enzymes, Inhibitors, and Substrates, Inhibitors, Membrane Protein Biology Tools, Merck, Modulators for MRP Transporters, Multi-Drug Resistance, Multi-Drug Resistance and Drug Metabolism, P, Proteins and Derivatives, Xenobiotics and Drug Metabolism, 细胞生物学
• {SNA} Application Index,

产品应用

• An inhibitor of several ABC-transporters of the subfamily ABCC or MRP.

相关文献及参考

• McKinney, S.E., et al.: J. Pharmacol. Exp. Ther., 102, 208 (1951),
• Israili, Z.H., et al.: J. Med. Chem., 15, 709 (1972),
• Al-Badr, A.A., et al.: Anal. Profiles Drug Subs., 10, 639 (1981),
• Short: III/10a Title: Structure Data of Organic Crystals: C ... C 15 Author: Schudt-Weitz, G.; Strell, I. Editor: Hellwege, K.-H.; Hellwege, A.M. Source: Landolt-Börnstein, New Series Volume: III/10a Year: 1985 ISBN: 3-540-07834-7 ISBN: 978-3-540-07834-0 Internet Resource: DOI:10.1007/b19984 RefComment: XXII, 634 pages. Hardcover Abstract: The volume includes an alphabetical index of all substances and a separate "ring index" with all cyclic compounds.
• Short: EINECS Title: EINECS (European Inventory of Existing Commercial Chemical Substances) Source: Official Journal of the European Communities Volume: C 146 A (15.06.1990) Page: 1 Year: 1990 Internet Resource: http://ecb.jrc.ec.europa.eu/esis/index.php?PGM=ein Publish_Date: 1990/06/15

安全信息

GHS Symbol

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 206 gm/kg/2Y-C
TOXIC EFFECTS :
   Tumorigenic - neoplastic by RTECS criteria
   Liver - tumors
REFERENCE :
   NTPTR* National Toxicology Program Technical Report Series.  (Research
   Triangle Park, NC 27709) No.206-  Volume(issue)/page/year: NTP-TR-395,1991

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 1666 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   NIIRDN Drugs in Japan (Ethical Drugs).  (Yakugyo Jiho Co., Ltd., Tokyo,
   Japan)  Volume(issue)/page/year: 6,735,1982

TYPE OF TEST            : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : 230 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   CLDND* Compilation of LD50 Values of New Drugs.  (J.R. MacDougal, Dept. of
   National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa,
   Ont., Canad

TYPE OF TEST            : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE       : Intravenous
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 458 mg/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   CLDND* Compilation of LD50 Values of New Drugs.  (J.R. MacDougal, Dept. of
   National Health and Welfare, Food and Drug Divisions, 35 John St., Ottawa,
   Ont., Canada)

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Human - man
DOSE/DURATION           : 50 mg/kg/1W-I
TOXIC EFFECTS :
   Blood - other hemolysis with or without anemia
REFERENCE :
   JRHUA9 Journal of Rheumatology.  (920 Yonge St., Suite 608, Toronto, Ont.,
   Canada)  V.1-    1974-  Volume(issue)/page/year: 13,208,1986

TYPE OF TEST            : LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 611 mg/kg
TOXIC EFFECTS :
   Details of toxic effects

TYPE OF TEST            : Sister chromatid exchange
TEST SYSTEM             : Rodent - hamster Ovary
DOSE/DURATION           : 5 mg/L
REFERENCE :
   NTPTR* National Toxicology Program Technical Report Series.  (Research
   Triangle Park, NC 27709) No.206-  Volume(issue)/page/year: NTP-TR-395,1991

其他信息

• 不良反应:1.消化道反应：主要表现为少数病人有食欲减退、恶心、呕吐、腹部不适等。 2.中枢神经反应及过敏反应：偶见头痛、面部潮红、发热和皮肤瘙痒、皮炎等过敏反应。 3.其他严重毒性反应：表现为极个别患者有出血、粒细胞减少、再障性贫血、肾病综合征、肝坏死等。丙磺舒属磺胺类药物，故对磺胺药过敏的患者禁用。孕妇、消化性溃疡、肝肾功能障碍患者要慎用。另外，服药时应大量饮水，并加服适量碳酸钠以防止产生尿结石。在服药期间应注意检查血象。
• 上游原料:重铬酸钠 --> 溴化钠 --> 正丙基溴 --> 对甲苯磺酰胺
• 用途二:抗痛风药。该品为有机酸，脂溶性强，自肾小管分泌排出，又很容易被回吸收。故在丙磺郐存在下，体内某些有机酸在肾小管的运转将受到抑制，减少其他有机酸的排泄。故用于治疗慢性痛风，安全有效。对急性痛风的疼痛和炎症无作用，不适用于急性痛风。
• Acros Organ
• MSDS 信息:4-[(Dipropylamino)sulfonyl]benzoic acid(57-66-9).msds
• 方法一:对甲苯磺酰胺经重铬酸钠氧化为对羧苯磺酰胺，再用溴丙烷进行烷基化反应，所得丙磺舒钠用乙酸酸化即得丙磺舒。
• 图谱信息:丙磺舒(57-66-9)红外图谱(IR1) 丙磺舒(57-66-9)红外图谱(IR2) 丙磺舒(57-66-9)质谱(MS)
• Probenecid
• 用途一:用于治疗痛风、慢性风湿性关节炎等疾病
• 适应证:(1)高尿酸血症伴慢性痛风性关节炎及痛风石，成人每日2次，每次25 mg，1周后可增量至每日2次，每次500 mg。服药时每日摄入水分2500mL左右，防止形成肾结石，必要时同服碱化尿液药物。但必须:1,肾小球滤过滤大于50～60mL/min;2,无肾结石或肾结石史;3,非酸性尿;4,不服用水杨酸类药物者;5,定期检测血和尿pH值、肝肾功能及血和尿中尿酸水平;6,根据临床及尿酸水平调整药量，用最小有效量维持较长时间。 (2)作为抗生素治疗的辅助用药，与青霉素、氨苄西林、苯唑西林、邻氯西林、萘夫西林(nafcillin)等抗生素同用时，丙磺舒可抑制这些抗生素的排出，提高血药浓度并能维持较长时间。
• Alfa Aesar:丙磺舒,98% Probenecid, 98%(57-66-9)
• 丙磺舒价格(试剂级):更新日期 产品编号 产品名称 包装 价格 2010/06/21 SB00915EE 丙磺舒 4-[(dipropylamino)sulfonyl]benzoic acid 50 GR 1275元 2010/06/21 SB00915EA 丙磺舒 4-[(dipropylamino)sulfonyl]benzoic acid 10 GR 405元 2010/06/21 SB00915EB 丙磺舒 4-[(dipropylamino)sulfonyl]benzoic acid 25 GR 795元
• Probenecid 是一种经典的有机阴离子运输竞争性抑制剂,同时也是一种瞬时感受器电位香草素受体亚家族2(TRPV2)的激动剂和人苦味觉感受器TAS2R16的抑制剂。
• Sigma Aldrich:57-66-9(sigmaaldrich)
• 抗痛风药:丙磺舒是一种化学合成的磺胺类抗痛风药，又叫羟苯磺胺，有促进尿酸排泄和抑制青霉素排泄的双重作用，临床上用于慢性痛风及抑制青霉素类药物的排泄以提高其血浆浓度，作为青霉素类治疗的辅助药。其作用机理为抑制肾小管对尿酸的重吸收，增加尿酸排泄，从而降低血浆中的尿酸浓度，以减少尿酸盐在组织中沉积，防止尿酸盐结晶的生成。本品亦可促进已形成的尿酸盐的溶解，从而减少关节的损伤。另外，本品还可以竞争性抑制弱有机酸(如青霉素、头孢菌素)在肾小管的分泌，从而可以增加这些抗生素的血浓度和延长它们的作用时间。本品口服易吸收，血浆蛋白结合率高达85%～90%。成人每次口服1g，2～4小时血药浓度即达峰值，半衰期为6～12小时。丙磺舒在肝内迅速代谢，主要代谢产物为丙磺舒乙酰葡萄醛酸。代谢物主要从尿中排泄。本品无抗炎镇痛作用，故对急性痛风无效。急性毒性试验结果：大鼠经口LD50为1600mg/kg。服后不良反应主要是胃肠
• MOL 文件:57-66-9.mol