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乙酰唑胺钠

乙酰唑胺钠用途

乙酰唑胺钠是乙酰唑酰胺的钠盐。乙酰唑胺是碳酸酐酶(CA)IX抑制剂,对hCA IX的IC50为30 nM。乙酰唑酰胺具有利尿、降压和抗淋菌活性[1][4][5][6]。
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乙酰唑胺钠名称

[ CAS 号 ]:
1424-27-7

[ 中文名 ]:
乙酰唑胺钠

[ 英文名 ]:
Acetazolamide

[英文别名 ]:

乙酰唑胺钠生物活性

[ 描述 ]:

乙酰唑胺钠是乙酰唑酰胺的钠盐。乙酰唑胺是碳酸酐酶(CA)IX抑制剂,对hCA IX的IC50为30 nM。乙酰唑酰胺具有利尿、降压和抗淋菌活性[1][4][5][6]。

[ 相关类别 ]:

研究领域 >> 感染
信号通路 >> 自噬 >> 自噬
信号通路 >> 代谢酶/蛋白酶 >> 碳酸酐酶
研究领域 >> 代谢疾病
信号通路 >> 抗感染 >> 细菌

[体外研究]

乙酰唑胺也抑制hCA II,IC50为130 nM[1]。乙酰唑胺(Ace)是一种小的杂芳磺酰胺,以高亲和力结合各种碳酸酐酶,作为碳酸酐酶(CA)抑制剂[2]。与对照组相比,高乙酰唑胺浓度(AceH,50 nM)、顺铂(Cis；1µg/mL)和Cis联合低乙酰唑酰胺浓度(AceL,10 nM)治疗显著降低了Hep-2细胞的活力[2]。与对照组相比,乙酰唑胺/顺式联合治疗显著增加P53的表达水平,因为AceL+顺式和AceH+顺式治疗均导致P53蛋白表达水平显著增加。与对照组相比,Ace/Cis联合治疗显著降低bcl-2/bax表达率,并增加caspase-3蛋白的表达。与对照组相比,AceL、AceH、Cis和AceL+Cis治疗显著降低bcl-2/bax比率[2]。Ace和Cis联合治疗可有效促进Hep-2细胞凋亡[2]。Ace/Cis联合治疗可显著降低Hep-2细胞中AQP1 mRNA的表达。与对照组相比,AceH和AceL+Cis处理均降低了Hep-2细胞中水通道蛋白-1(AQP1)mRNA的表达[2]。

[体内研究]

乙酰唑胺(40 mg/kg)显著增强MS-275对神经母细胞瘤(NB)SH-SY5Y异种移植物肿瘤发生的抑制作用[3]。乙酰唑胺(40 mg/kg)和/或MS-275治疗可降低NB SH-SY5Y异种移植物中HIF1-α和CAIX的表达[3]。乙酰唑胺(40 mg/kg)、MS-275和乙酰唑酰胺+MS-275降低NB SH-SY5Y异种移植物中有丝分裂和增殖标记物的表达[3]。乙酰唑胺(50 mg/kg；PO,持续3天)显著降低感染小鼠阴道内淋菌负荷90%[6]。

[参考文献]

[1]. Bayat Mokhtari R, et al. Acetazolamide potentiates the anti-tumor potential of HDACi, MS-275, in neuroblastoma. BMC Cancer. 2017 Feb 24;17(1):156.

[2]. Hou Z, et al. Dual-tail approach to discovery of novel carbonic anhydrase IX inhibitors by simultaneously matching the hydrophobic and hydrophilic halves of the active site. Eur J Med Chem. 2017 May 26;132:1-10.

[3]. Gao H, et al. Combined treatment with acetazolamide and cisplatin enhances chemosensitivity in laryngeal carcinoma Hep-2 cells. Oncol Lett. 2018 Jun;15(6):9299-9306.

[4]. Kassamali R, et al. Acetazolamide: a forgotten diuretic agent. Cardiol Rev. 2011 Nov-Dec;19(6):276-8.

[5]. Jabeen E, et al. Interaction of antihypertensive acetazolamide with nonsteroidal anti-inflammatory drugs. J Photochem Photobiol B. 2013 Aug 5;125:155-63.

[6]. Abutaleb NS, et al. In vivo efficacy of acetazolamide in a mouse model of Neisseria gonorrhoeae infection. Microb Pathog. 2022 Mar;164:105454.

乙酰唑胺钠物理化学性质

[ 熔点 ]:
258-259ºC (EFFERVESCENCE)

[ 分子式 ]:
C4H5N4NaO3S2

[ 分子量 ]:
244.22700

[ 精确质量 ]:
243.97000

[ PSA ]:
142.87000

[ LogP ]:
0.78380

[ 外观性状 ]:
固体

[ 储存条件 ]:
库房通风低温干燥

乙酰唑胺钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AC8400000
CHEMICAL NAME :
Acetamide, N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-, monosodium salt
CAS REGISTRY NUMBER :
1424-27-7
LAST UPDATED :
199609
DATA ITEMS CITED :
20
MOLECULAR FORMULA :
C4-H5-N4-O3-S2.Na
MOLECULAR WEIGHT :
244.24
WISWESSER LINE NOTATION :
T5NN DSJ CSZW EMV1 &-NA-

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
TYPE OF TEST :
LD - Lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
1500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
1 gm/kg/10D-I
TOXIC EFFECTS :
Nutritional and Gross Metabolic - changes in sodium Nutritional and Gross Metabolic - changes in potassium
REFERENCE :
JHHBAI Bulletin of the Johns Hopkins Hospital. (Baltimore, MD) V.1-119, 1889-1966. For publisher information, see JHMJAX. Volume(issue)/page/year: 95,199,1954 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
1 gm/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
1 gm/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
850 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 28,355,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
1 gm/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 10,221,1974
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
200 mg/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)
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: 27,51,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
1 gm/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
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: 28,45,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
3 gm/kg
SEX/DURATION :
female 9-11 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death
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: 28,45,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
200 mg/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 28,45,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
1500 mg/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - cytological changes (including somatic cell genetic material)
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: 15,199,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
1500 mg/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 15,199,1977
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
300 mg/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 4,95,1971
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
600 mg/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - Central Nervous System
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: 4,95,1971
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravaginal
DOSE :
110 mg/kg
SEX/DURATION :
female 8 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - musculoskeletal system
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: 7,209,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5616 No. of Facilities: 17 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 223 (estimated) No. of Female Employees: 137 (estimated)
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[ 危害码 (欧洲) ]:
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【乙酰唑胺钠】化源网提供乙酰唑胺钠CAS号1424-27-7，乙酰唑胺钠MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询乙酰唑胺钠上化源网，专业又轻松。>>电脑版：乙酰唑胺钠

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