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磺胺

磺胺用途

Sulfanilamide是细菌二氢蝶酸合成酶抑制剂,IC50为320 μM。

磺胺名称

[ CAS 号 ]:
63-74-1

[ 中文名 ]:
磺胺

[ 英文名 ]:
Sulfanilamide

[中文别名 ]:

[英文别名 ]:

EINECS 200-563-4
Sulphonamide
Sulfamine
MFCD00007939
Sulfanilamide
Sulfonylamide
4-aminobenzene sulfonic acid amide
4-aminobenzene sulfonamide
4-aminobenzenesulfonamide
Bacteramid

磺胺生物活性

[ 描述 ]:

Sulfanilamide是细菌二氢蝶酸合成酶抑制剂,IC50为320 μM。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[参考文献]

[1]. McCullough, J.L. and T.H. Maren, Inhibition of dihydropteroate synthetase from Escherichia coli by sulfones and sulfonamides. Antimicrob Agents Chemother, 1973. 3(6): p. 665-9.

[2]. Meneau, I., et al., Pneumocystis jiroveci dihydropteroate synthase polymorphisms confer resistance to sulfadoxine and sulfanilamide in Saccharomyces cerevisiae. Antimicrob Agents Chemother, 2004. 48(7): p. 2610-6.

[3]. Hughes, W.T. and J. Killmar, Monodrug efficacies of sulfonamides in prophylaxis for Pneumocystis carinii pneumonia. Antimicrob Agents Chemother, 1996. 40(4): p. 962-5.

[相关活性小分子]

磺胺物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
400.5±47.0 °C at 760 mmHg

[ 熔点 ]:
164-166 °C(lit.)

[ 分子式 ]:
C₆H₈N₂O₂S

[ 分子量 ]:
172.205

[ 闪点 ]:
196.0±29.3 °C

[ 精确质量 ]:
172.030655

[ PSA ]:
94.56000

[ LogP ]:
-0.72

[ 外观性状 ]:
白色至淡黄色结晶粉末

[ 蒸汽压 ]:
0.0±0.9 mmHg at 25°C

[ 折射率 ]:
1.628

[ 储存条件 ]:
包装完整、轻装轻放,库房通风、远离明火、高温、与氧化剂分开存放

[ 水溶解性 ]:
7.5 g/L at 25 ºC

磺胺MSDS

磺胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WO8400000

CHEMICAL NAME :: Sulfanilamide

CAS REGISTRY NUMBER :: 63-74-1

BEILSTEIN REFERENCE NO. :: 0511852

LAST UPDATED :: 199701

DATA ITEMS CITED :: 30

MOLECULAR FORMULA :: C6-H8-N2-O2-S

MOLECULAR WEIGHT :: 172.22

WISWESSER LINE NOTATION :: ZSWR DZ

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 :: 3900 mg/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 :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1400 mg/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 :: 3 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 :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5 mg/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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2900 mg/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 :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/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 :: Mammal - dog

DOSE/DURATION :: 2 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 - rabbit

DOSE/DURATION :: 1300 mg/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 - guinea pig

DOSE/DURATION :: 3130 mg/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 :: 180 gm/kg/90D-I

TOXIC EFFECTS :: Blood - changes in spleen Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 82200 mg/kg/39W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - other changes

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 60 gm/kg/30D-I

TOXIC EFFECTS :: Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 135 mg/kg/9W-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Tumorigenic - tumors at site of application

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

DOSE :: 974 mg/kg

SEX/DURATION :: female 34-37 week(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - blood and lymphatic systems (including spleen and marrow)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 22 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 22 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: DNA damage

TEST SYSTEM :: Rodent - rat Liver

DOSE/DURATION :: 30 umol/L

REFERENCE :: SinJF# Personal Communication from J.F. Sina, Merck Institute for Therapeutic Research, West Point, PA 19486, Oct. 26, 1982 Volume(issue)/page/year: 26OCT1982 *** REVIEWS *** TOXICOLOGY REVIEW JMSHAO Journal of the Mount Sinai Hospital (New York). (New York, NY) V.1-36, 1934-69. For publisher information, see MSJMAZ. Volume(issue)/page/year: 10,343,1943 TOXICOLOGY REVIEW PCNAA8 Pediatric Clinics of North America. (W.B. Saunders Co., W. Washington Sq., Philadelphia, PA 19105) V.1- 1954- Volume(issue)/page/year: 8,413,1961 TOXICOLOGY REVIEW DPIRDU Dangerous Properties of Industrial Materials Report. (Van Nostrand Reinhold, 115 Fifth Ave., New York, NY 10003) V.1- 1981- Volume(issue)/page/year: 2(6),13,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84382 No. of Facilities: 149 (estimated) No. of Industries: 3 No. of Occupations: 9 No. of Employees: 3565 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 84382 No. of Facilities: 654 (estimated) No. of Industries: 6 No. of Occupations: 11 No. of Employees: 6529 (estimated) No. of Female Employees: 3131 (estimated)

磺胺安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R40

[ 安全声明 (欧洲) ]:
S24/25

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

[ WGK德国 ]:
3

[ RTECS号 ]:
WO8400000

[ 海关编码 ]:
2935009090

磺胺合成路线

磺胺上下游产品

磺胺上游产品

磺胺下游产品

磺胺制备

1.由乙酰苯胺经氯磺化、胺化、水解、中和制得。
原料消耗定额：乙酰苯胺（99%）1032kg/t、氯磺酸（96%）4521kg/t、液氨（99.8%）535kg/t、

液碱（30%）863kg/t。

磺胺海关

[ 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%

磺胺文献

Enhanced antioxidant capacity of dental pulp-derived iPSC-differentiated hepatocytes and liver regeneration by injectable HGF-releasing hydrogel in fulminant hepatic failure.

Cell. Transplant. 24(3) , 541-59, (2015)

Acute hepatic failure (AHF) is a severe liver injury leading to sustained damage and complications. Induced pluripotent stem cells (iPSCs) may be an alternative option for the treatment of AHF. In thi...

Carbonic anhydrase inhibitors. Inhibition studies with anions and sulfonamides of a new cytosolic enzyme from the scleractinian coral Stylophora pistillata.

Bioorg. Med. Chem. Lett. 21 , 710-4, (2011)

The catalytic activity and the inhibition of a new coral carbonic anhydrase (CA, EC 4.2.1.1), from the scleractinian coral Stylophora pistillata, STPCA-2, has been investigated. STPCA-2 has high catal...

Down regulation of NO signaling in Trypanosoma cruzi upon parasite-extracellular matrix interaction: changes in protein modification by nitrosylation and nitration.

PLoS Negl. Trop. Dis. 9 , e0003683, (2015)

Adhesion of the Trypanosoma cruzi trypomastigotes, the causative agent of Chagas' disease in humans, to components of the extracellular matrix (ECM) is an important step in host cell invasion. The sig...

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磺胺