氯塞酮

氯塞酮

中文名称氯塞酮
中文同义词2-氯-5-(2,3-二氢-1-羟基-3-氧代-1H-异吲哚-1-基)苯磺酰胺;氯塞酮;氯塞酮/2-氯-5-(2,3-二氢-1-羟基-3-氧代-1H-异吲哚-1-基)苯磺酰胺;氯塞酮(氯噻酮);氯噻酮;氯噻酮溶液,100PPM;氯噻酮溶液,1000PPM;氯吡酮杂质
英文名称Chlortalidone
英文同义词thalitone;2-chloro-5-(2,3-dihydro-1-hydroxy-3-oxo-1h-isoindol-1-yl)benzenesulfonamide;hygroton;CHLORTHALIDONE;CHLORTALIDONE;1-keto-3-(3’-sulfamyl-4’-chlorophenyl)-3-hydroxyisoindoline;1-oxo-3-(3-sulfamyl-4-chlorophenyl)-3-hydroxyisoindoline;2-chloro-5-(1-hydroxy-3-oxo-1-isoindolinyl)-benzenesulfonamid
CAS号77-36-1
分子式C14H11ClN2O4S
分子量338.77
EINECS号201-022-5
相关类别原料药;小分子抑制剂;无机化合物和盐;有机化学;有机中间体;医药原料药-科研原料;农药原料;原料;Amines;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;CHForensic and Veterinary Standards;Alphabetic;C;Drugs&Metabolites;Neat Compounds;THALITONE;医用原料;试剂盒-Elisa试剂盒;化学试剂
Mol文件77-36-1.mol
结构式氯塞酮 结构式

氯塞酮 性质

熔点265-267°C (dec.)
密度1.3356 (rough estimate)
折射率1.5630 (estimate)
储存条件2-8°C
溶解度DMSO:可溶5mg/mL,澄清(加热)
酸度系数(pKa)pKa 9.4 (Uncertain)
形态粉末
颜色白色至米色
水溶解性0.12g/L(25 ºC)
稳定性吸湿性
InChIKeyJIVPVXMEBJLZRO-UHFFFAOYSA-N
NIST化学物质信息Chlorthalidone(77-36-1)
EPA化学物质信息Benzenesulfonamide, 2-chloro-5-(2,3-dihydro-1-hydroxy-3-oxo-1H-isoindol-1-yl)- (77-36-1)

氯塞酮 用途与合成方法

Chlortalidone (Chlortalidone)是一种利尿剂,用于治疗高血压。

Chlorthalidone通过抑制钠离子通过肾小管上皮细胞的转运,增加钠,氯,和水排泄到肾内腔。它作用的主要位点是髓袢上升支的皮质稀释段。通过增加钠到远端肾小管的转运,chlorthalidone通过钠钾交换机制间接增加钾分泌(即顶端ROMK/Na 通道耦合基底侧NKATPases)。

Chlorthalidone is a thiazide-like diuretic. After oral intake, peak serum concentrations are achieved in 2-6 hours. The half-life of Chlorthalidone is approximately 42 (range 29-55) hours, reaching 45-60 hours after long-term dosing. However, interindividual variability in the half-life of Chlorthalidone is wide. Chlorthalidone is excreted unchanged by the kidneys. The natriuretic effect of Chlorthalidone is maximal at 18 hours and lasts more than 48 hours. Comparing different doses of Chlorthalidone, it has been observed that 25 mg daily is nearly as effective as higher doses, but with less risk of hypokalemia. Chlorthalidone reduces calcium oxalate calculous recurrence but magnesium hydroxide does not. The effectiveness of Chlorthalidone or magnesium hydroxide is examined in the prevention of recurrent calcium oxalate kidney calculi. In a double-blind random allocation design daily dosages of 25 or 50 mg. Chlorthalidone, 650 or 1,300 mg. magnesium hydroxide, or an identical placebo are administered. All groups showed significantly decreased calculous events compared to the pretreatment rates. During the trial 56.1 per cent fewer calculi than predicted developed in the placebo group (p less than 0.01), whereas the groups receiving low and high dosage magnesium hydroxide showed 73.9 and 62.3 per cent fewer calculi, respectively (p less than 0.001 and less than 0.01, respectively). Chlorthalidone treatment results in a 90.1 per cent decrease from predicted rates and both dosages yielded similar results. When the treatments are compared Chlorthalidone is significantly better than the placebo or magnesium hydroxide (p less than 0.01). The large decreases in calculous events seen when placebo or ineffective therapy is given underscore the positive treatment bias that occurs when historical controls are used and they demonstrate the need for proper experimental design.

化学性质 
白色结晶性粉末。熔点224-226℃(分解)。微溶于水、乙醇、氯仿,溶于热乙醇。无臭,无味。
用途 
利尿药,用于心脏性,肾性及其他水肿病。
生产方法 
由2-(3-氨基-4-氯苯甲酰)苯甲酸[118-04-7]经重氮化、置换、氯磺化、环合、胺化而得。

安全信息

安全说明22-24/25
WGK Germany2
RTECS号DB1556000
海关编码2935904000
毒害物质数据77-36-1(Hazardous Substances Data)
毒性LD50 oral in rabbit: > 5gm/kg

MSDS信息

提供商 语言
英文
更新日期产品编号产品名称CAS号包装价格
2024/01/25HY-15833氯塞酮
Chlorthalidone
77-36-150mg200元
2024/01/25HY-15833氯塞酮
Chlorthalidone
77-36-110mM * 1mLin DMSO220元
"氯塞酮"相关产品信息
对氯苯乙酮 邻甲酸甲酯苯磺酰胺 芬那露 2,6-二甲基-7-辛烯-2-醇 对甲苯磺酰胺 结晶磺胺 曲唑酮 苯磺酰胺 偶氮氯磷 甲基磺酰胺 氯氨酮 邻羟基氯苄 盐酸氯普噻吨 氯噻酮 氯代醚酮 一氯二氟甲烷 氯塞酮 氯噻酮
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