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依索唑胺

依索唑胺用途

Ethoxzolamide 是 carbonic anhydrase 的抑制剂,其 Ki 值为 1 nM。

依索唑胺名称

[ CAS 号 ]:
452-35-7

[ 中文名 ]:
依索唑胺

[ 英文名 ]:
Ethoxzolamide

[中文别名 ]:

[英文别名 ]:

Ethamide
6-ethoxy-1,3-benzothiazole-2-sulfonamide
Glaucotensil
Ethoxyzolamide
Ethoxazolamide
2-Benzothiazolesulfonamide,6-ethoxy
EINECS 207-199-5
MFCD00057089
Etoxzolamide
6-Ethoxy-2-benzothiazolesulfonamide

依索唑胺生物活性

[ 描述 ]:

Ethoxzolamide 是 carbonic anhydrase 的抑制剂,其 Ki 值为 1 nM。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 碳酸酐酶

研究领域 >> 炎症/免疫

研究领域 >> 感染

[ 靶点 ]

Ki: 1 nM (carbonic anhydrase)[1]

[体外研究]

乙氧唑胺(ETZ)处理在受感染的巨噬细胞中引起> 90％的报告基因GFP荧光抑制。此外,在9天巨噬细胞存活试验中,乙氧唑胺(ETZ)处理显着抑制结核分枝杆菌在细胞内生长的能力[2]。

[体内研究]

发现脂溶性乙氧唑胺在体内转化为水溶性代谢物,同时保持对酶的高活性。在最大效应的最小剂量(45分钟静脉内4mg/kg)下,IOP降低为4.2mmHg,前葡萄膜中的浓度为2.5pmol/kg,酶(i)的分数抑制为0.9995。由于血浆中药物的半衰期非常短,导致前葡萄膜和其他组织中游离药物的消耗[1],因此效果迅速下降。乙氧唑胺(ETZ)强烈下调小鼠肺中的GFP报告荧光,与模拟处理对照相比,GFP信号抑制3倍。与模拟处理对照相比,ETZ处理小鼠的肺中细菌存活率显着降低[2]。

[细胞实验]

每2天用80μM乙氧唑胺（ETZ）或等体积的DMSO处理BMDM，共9天。在第3,6和9天，通过裂解巨噬细胞单层并在7H10琼脂上进行裂解物的连续稀释平板来定量细胞内细菌。对于荧光显微镜实验，在感染结核分枝杆菌CDC1551之前，将巨噬细胞接种在玻璃盖玻片上。每隔2天用100μM乙氧唑胺（ETZ）或等体积的DMSO处理样品9天[2]。

[动物实验]

将大鼠（雄性，300-325g）随机分成2组（每组n = 6），并以0.18mg / kg（PEG 300：乙醇，1：1）的剂量通过静脉注射给予乙氧唑胺（EZ）。通过尾静脉注射。在注射后0,15,30,60,120,180,240,360,540和1440分钟通过尾部剪切以异氟烷作为麻醉剂，在肝素化管中收集血液样品（约50-100μL）。制备血浆样品并储存在-80℃直至分析。为了研究脑中的分布，第1组中的大鼠在6小时时被瘢痕化，第2组中的大鼠在24小时时被瘢痕化以收集脑组织。分析来自第2组的那些血液样品以产生PK曲线[3]。

[参考文献]

[1]. Maren TH, et al. Relations among IOP reduction, ocular disposition and pharmacology of the carbonic anhydrase inhibitor ethoxzolamide. Exp Eye Res. 1992 Jul;55(1):73-9.

[2]. Benjamin K. Johnson, et al. The Carbonic Anhydrase Inhibitor Ethoxzolamide Inhibits theMycobacterium tuberculosis PhoPR Regulon and Esx-1 Secretion and Attenuates Virulence. Antimicrob Agents Chemother. 2015 Aug; 59(8): 4436–4445.

[3]. Song Gao, et al. Development and validation of an UPLC-MS/MS method for the quantification of ethoxzolamide in plasma and bioequivalent buffers: Applications to absorption, brain distribution, and pharmacokinetic studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Apr 1; 0: 54–59.

[相关活性小分子]

依索唑胺物理化学性质

[ 密度 ]:
1.47g/cm3

[ 沸点 ]:
464.9ºC at 760mmHg

[ 熔点 ]:
190-193ºC(lit.)

[ 分子式 ]:
C₉H₁₀N₂O₃S₂

[ 分子量 ]:
258.31700

[ 闪点 ]:
235ºC

[ 精确质量 ]:
258.01300

[ PSA ]:
118.90000

[ LogP ]:
3.12350

[ 蒸汽压 ]:
8.05E-09mmHg at 25°C

[ 折射率 ]:
1.644

[ 储存条件 ]:
2-8℃

依索唑胺MSDS

详细MSDS(安全技术说明书)

依索唑胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DL6390000

CHEMICAL NAME :: 2-Benzothiazolesulfonamide, 6-ethoxy-

CAS REGISTRY NUMBER :: 452-35-7

BEILSTEIN REFERENCE NO. :: 0212240

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C9-H10-N2-O3-S2

MOLECULAR WEIGHT :: 258.33

WISWESSER LINE NOTATION :: T56 BN DSJ CSZW GO2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3300 mg/kg

SEX/DURATION :: female 1-22 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 1,51,1968

依索唑胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
DL6390000

[ 海关编码 ]:
2935009090

依索唑胺合成路线

详细合成路线

依索唑胺上下游产品

依索唑胺上游产品

依索唑胺下游产品

依索唑胺海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

依索唑胺文献

Transport activity of the sodium bicarbonate cotransporter NBCe1 is enhanced by different isoforms of carbonic anhydrase.

PLoS ONE 6(11) , e27167, (2011)

Transport metabolons have been discussed between carbonic anhydrase II (CAII) and several membrane transporters. We have now studied different CA isoforms, expressed in Xenopus oocytes alone and toget...

Reversed electrogenic sodium bicarbonate cotransporter 1 is the major acid loader during recovery from cytosolic alkalosis in mouse cortical astrocytes.

J. Physiol. 593 , 3533-47, (2015)

The regulation of H(+) i from cytosolic alkalosis has generally been attributed to the activity of Cl(-) -coupled acid loaders/base extruders in most cell types, including brain cells. The present stu...

Functional interaction between bicarbonate transporters and carbonic anhydrase modulates lactate uptake into mouse cardiomyocytes.

Pflugers Arch. 467 , 1469-80, (2015)

Blood-derived lactate is a precious energy substrate for the heart muscle. Lactate is transported into cardiomyocytes via monocarboxylate transporters (MCTs) together with H(+), which couples lactate ...

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