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氯尼达明

氯尼达明用途

Lonidamine是口服活性的己糖激酶抑制剂。

氯尼达明名称

[ CAS 号 ]:
50264-69-2

[ 中文名 ]:
氯尼达明

[ 英文名 ]:
Lonidamine

[中文别名 ]:

[英文别名 ]:

DICA
Lonidaminum
Lonidamin
Lonidaminum [INN-Latin]
MFCD00866285
Diclondazolic acid
Lonidamine
EINECS 256-510-0
Lonidamina
Doridamina

氯尼达明生物活性

[ 描述 ]:

Lonidamine是口服活性的己糖激酶抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 己糖激酶

研究领域 >> 癌症

[参考文献]

[1]. http://en.wikipedia.org/wiki/Lonidamine

[相关活性小分子]

2-脱氧-D-葡萄糖 | 3-溴丙酮酸

氯尼达明物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
537.9±45.0 °C at 760 mmHg

[ 熔点 ]:
207-209°C

[ 分子式 ]:
C₁₅H₁₀Cl₂N₂O₂

[ 分子量 ]:
321.158

[ 闪点 ]:
279.1±28.7 °C

[ 精确质量 ]:
320.011932

[ PSA ]:
55.12000

[ LogP ]:
4.32

[ 外观性状 ]:
白色至淡黄色晶体

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.678

[ 储存条件 ]:
Store at RT

氯尼达明MSDS

氯尼达明毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NK7886000

CHEMICAL NAME :: 1H-Indazole-3-carboxylic acid, 1-(2,4-dichlorobenzyl)-

CAS REGISTRY NUMBER :: 50264-69-2

BEILSTEIN REFERENCE NO. :: 0894483

LAST UPDATED :: 199612

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C15-H10-Cl2-N2-O2

MOLECULAR WEIGHT :: 321.17

WISWESSER LINE NOTATION :: T56 BNNJ B1R BG DG& DVQ

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 :: 1700 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay)

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 525 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay)

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 900 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay)

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 435 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Behavioral - changes in motor activity (specific assay)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14560 mg/kg/2Y-C

TOXIC EFFECTS :: Related to Chronic Data - changes in testicular weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3 gm/kg/30D-I

TOXIC EFFECTS :: Related to Chronic Data - changes in prostate weight Related to Chronic Data - changes in testicular weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 3200 mg/kg/28D-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 35 mg/kg

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

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 350 mg/kg

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

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 175 mg/kg

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

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 90 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 100 mg/kg

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

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 250 mg/kg

SEX/DURATION :: male 5 day(s) pre-mating

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

TYPE OF TEST :: Sperm Morphology

MUTATION DATA

TEST SYSTEM :: Primate - monkey

DOSE/DURATION :: 250 mg/kg/5D

REFERENCE :: JRPFA4 Journal of Reproduction and Fertility. (Biochemical Soc. Book Depot, POB 32, Commerce Way, Colchester, Essex CO2 8HP, UK) V.1- 1960- Volume(issue)/page/year: 52,275,1978

氯尼达明安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H302-H351-H360

[ 警示性声明 ]:
P201-P281-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R60;R22;R40

[ 安全声明 (欧洲) ]:
S53-S22-S36/37/39-S45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
NK7886000

[ 海关编码 ]:
2933990090

氯尼达明合成路线

氯尼达明上下游产品

氯尼达明上游产品

氯尼达明下游产品

氯尼达明制备

吲哚醌加入氢氧化钠的水溶液中,水解开环得到化合物(I).将化合物(I)在0℃和亚硝酸钠水溶液混合,再将该混合液滴入硫酸水溶液中，保持在4℃以下,滴完继续搅拌得重氮盐溶液.于0℃和搅拌下,滴入氯化亚锡的浓盐酸溶液,继续搅拌.过滤得黄棕色固体,冰醋酸重结晶得黄色针状的吲唑-3-羧酸(Ⅲ)的结晶,收率,51.2%.

将该吲唑羧酸、氢氧化钠、水和碘化钾一起,在氮气保护下,在100℃和搅拌下,缓慢滴加2,4-二氯苄基氯,加毕继续反应.滤集晶体,用乙醇重结晶,得氯尼达明,收率87.5%,熔点205～206℃.

其最后一步反应也可如下进行：1H-吲脞-3-羧酸溶于8g氢氧化钠和160ml水的溶液中,在水浴加热及搅拌下加入2,4-二氯苄基氯,加毕继续加热3h,冷却,用稀盐酸调至酸性,沉淀出的粗氯尼达明用醋酸重结晶,收率,70%,熔点207℃。

氯尼达明海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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