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硝呋替莫

硝呋替莫用途

Nifurtimox 是一种用于治疗锥虫病 (Trypanosoma cruzi) 的抗虫剂。Nifurtimox 可用于治疗神经母细胞瘤细胞。Nifurtimox 影响乳酸脱氢酶 (LDH) 活性。

硝呋替莫名称

[ CAS 号 ]:
23256-30-6

[ 中文名 ]:
硝呋替莫

[ 英文名 ]:
Nifurtimox

[中文别名 ]:

硝呋莫司

[英文别名 ]:

EINECS 245-531-0
Lampit
Nifurtimoxum [INN-Latin]
Bayer 2502
BAY 2502
Nifurtimox [INN:BAN]
NIFURTIMOX

硝呋替莫生物活性

[ 描述 ]:

Nifurtimox 是一种用于治疗锥虫病 (Trypanosoma cruzi) 的抗虫剂。Nifurtimox 可用于治疗神经母细胞瘤细胞。Nifurtimox 影响乳酸脱氢酶 (LDH) 活性。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 乳酸脱氢酶

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

研究领域 >> 癌症

[ 靶点 ]

Trypanosoma cruzi[1] Lactate dehydrogenase (LDH) [1]

[体外研究]

Nifurtimox影响乳酸脱氢酶(LDH)的酶活性。为了区分该效应是否是由于PDH活化导致的LDH活性降低或丙酮酸代谢的变化,在用50μg/ mL Nifurtimox处理4小时后测定LDH的酶活性。与未处理对照相比,LA-N-1(P = 0.005),IMR-32(P = 0.009),LS(P = 0.0035)和SK-N-SH(P = 0.0065)的LDH活性显着降低。 Nifurtimox降低神经母细胞瘤细胞的细胞活力并诱导细胞周期停滞和细胞凋亡。为了表征Nifurtimox对神经母细胞瘤的细胞毒性影响,对4种细胞系进行了几次实验。在用50μg/ mL孵育24小时后,所有4种神经母细胞瘤细胞系的细胞活力均降低至平均66％,63％,62％和75％(LA-N-1,IMR-32 LS和SK-N-) SH,分别)。与未处理的对照(P <0.01)和用DMSO的载体对照(P <0.05)相比,所有细胞系的减少都是显着的[1]。

[细胞实验]

神经母细胞瘤细胞系IMR-32，LA-N-1和SK-N-SH以及神经母细胞瘤细胞系LS在补充有10％（v / v）胎牛血清（FCS）的RPMI-1640培养基中生长，2mM L-谷氨酰胺，100U / mL青霉素和100μg/ mL链霉素，并在37℃，5％CO 2和饱和湿度下孵育。为了评估与Nifurtimox在不同浓度（10μg/ mL至50μg/ mL或34.8μM至174μM，分别在上清液生长培养基中）或具有相应浓度的载体对照孵育后的细胞活力，所有神经母细胞瘤细胞系均为进行MTS测定。 MTS的储备溶液在无菌过滤的去离子水中以480μM制备并储存在-20℃。细胞生长至约50％汇合，用Nifurtimox处理，并与含有12μMMTS的新鲜培养基一起孵育1小时[1]。

[参考文献]

[1]. Cabanillas Stanchi KM, et al. Nifurtimox reduces N-Myc expression and aerobic glycolysis in neuroblastoma. Cancer Biol Ther. 2015;16(9):1353-63.

[相关活性小分子]

硝呋替莫物理化学性质

[ 密度 ]:
1.56g/cm3

[ 沸点 ]:
550.3ºC at 760mmHg

[ 分子式 ]:
C₁₀H₁₃N₃O₅S

[ 分子量 ]:
287.29200

[ 闪点 ]:
286.6ºC

[ 精确质量 ]:
287.05800

[ PSA ]:
117.08000

[ LogP ]:
2.18250

[ 蒸汽压 ]:
3.7E-12mmHg at 25°C

[ 折射率 ]:
1.653

[ 储存条件 ]:
2-8℃

硝呋替莫MSDS

详细MSDS(安全技术说明书)

硝呋替莫毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XM3020000

CHEMICAL NAME :: Thiomorpholine, 3-methyl-4-((5-nitrofurfurylidene)amino)-, 1,1-dioxide

CAS REGISTRY NUMBER :: 23256-30-6

LAST UPDATED :: 199706

DATA ITEMS CITED :: 25

MOLECULAR FORMULA :: C10-H13-N3-O5-S

MOLECULAR WEIGHT :: 287.32

WISWESSER LINE NOTATION :: T6N DSWTJ B1 ANU1- BT5OJ ENW

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 :: 4050 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2291 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >800 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 :: Behavioral - convulsions or effect on seizure threshold Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - cat

DOSE/DURATION :: >4 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - nausea or vomiting

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 2 gm/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 :: 11700 mg/kg/47W-I

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Endocrine - adrenal cortex tumors Skin and Appendages - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 11700 mg/kg/47W-I

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Endocrine - thyroid tumors Skin and Appendages - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2520 mg/kg

SEX/DURATION :: male 70 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - male fertility index (e.g. # males impregnating females per # males exposed to fertile nonpregnant females)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 500 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 9100 mg/kg

SEX/DURATION :: male 91 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 mg/kg

SEX/DURATION :: male 1 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1250 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3136 mg/kg

SEX/DURATION :: male 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2 gm/kg

SEX/DURATION :: male 8 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

TYPE OF TEST :: Specific locus test

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sperm Morphology

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TEST SYSTEM :: Rodent - mouse

DOSE/DURATION :: 2 gm/kg

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 188,129,1987

硝呋替莫安全信息

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

硝呋替莫合成路线

详细合成路线

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硝呋替莫文献

Trypanocidal Activity of Long Chain Diamines and Aminoalcohols.

Molecules 20 , 11554-68, (2015)

Thirteen aminoalcohols and eight diamines were obtained and tested against Trypanosoma cruzi epimastigotes strains MG, JEM and CL-B5 clone. Some of them were equal or more potent (1.0-6.6 times) than ...

American Trypanosomiasis (Chagas Disease)

Infect. Dis. Clin. North Am. 26(2) , 275-91, (2012)

Chagas disease, also known as American trypanosomiasis, is a chronic infection caused by Trypanosoma cruzi, a protozoan parasite. It is transmitted to human beings mainly through the feces of infected...

Targeting the substrate preference of a type I nitroreductase to develop antitrypanosomal quinone-based prodrugs.

Antimicrob. Agents Chemother. 56(11) , 5821-30, (2012)

Nitroheterocyclic prodrugs are used to treat infections caused by Trypanosoma cruzi and Trypanosoma brucei. A key component in selectivity involves a specific activation step mediated by a protein hom...

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