规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5mg |
|
||
10mg |
|
||
Other Sizes |
|
药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
IN CHRONIC TOXICITY STUDIES ... LINURON ... CONTINUOUSLY FED TO RATS & DOGS FOR ... TWO YR AT DIETARY LEVELS ... FROM 25 TO 2500 PPM ... TOTAL ANILINE-CONTAINING RESIDUES IN BLOOD & ... (MUSCLE, FAT, LIVER, KIDNEY, SPLEEN) WERE A FEW TO 100 PPM. ... RESIDUES REPRESENTED ONLY MINUTE FRACTION OF ... HERBICIDE INGESTED BY ANIMALS. LINURON IS MOST READILY ABSORBED THROUGH THE ROOT SYSTEM; LESS SO THROUGH FOLIAGE & STEMS. HOWEVER, FOLIAR ABSORPTION ... IS SIGNIFICANTLY GREATER THAN THAT OF DIURON, MONURON, OR FENURON. ... TRANSLOCATION IS PRIMARILY UPWARD IN THE XYLEM. ... RESIDUE DATA ... OBTAINED IN SHORT TERM ELIMINATION EXPERIMENTS ... . AMT OFRADIOACTIVITY WHICH PERSISTED IN BLOOD & DIFFERENT TISSUES AT END OF 72 HR ... PERIODS WERE NO MORE & USUALLY MUCH LESS THAN 1% OF DOSE APPLIED. Metabolism / Metabolites ... LINURON-INDUCIBLE ENZYME WAS OBTAINED FROM BACILLUS SPHAERICUS. THIS ACYLAMIDASE DEGRADED LINURON BY HYDROLYSIS OF AMIDE BOND WITH ... RELEASE OF CARBON DIOXIDE & N,O-DIMETHYL HYDROXYLAMINE. ... ENZYME WAS SPECIFIC FOR METHOXY-SUBSTITUTED PHENYLUREAS & DID NOT HYDROLYZE 1,1-DIMETHYL PHENYLUREAS ... . IN GREENHOUSE STUDIES, LINURON ENTERED CORN (ZEA MAYS L), SOYBEAN (GLYCINE MAX L) & CRABGRASS (DIGITARIA SANGUINALIS L) WITH ABSORBED WATER. DEMETHYL LINURON & 3,4-DICHLORO-ANILINE WERE FOUND IN TISSUES. ... SOME LINURON BOUND WITHIN PLANT ... . LINURON ... FED TO ALBINO RATS. URINE ... ANALYZED FOR METABOLITES /&/ N-(3,4-DICHLOROPHENYL)UREA, N-(3,4-DICHLOROPHENYL)-N'-METHYLUREA & 3,4-DICHLOROANILINE WERE FOUND FREE. N-(2-HYDROXY-4,5-DICHLOROPHENYL)-N'-METHYLUREA, N-(5-HYDROXY-3,4-DICHLOROPHENYL)UREA & 6-ACETAMIDO-2,3-DICHLOROPHENOL ... /WERE IDENTIFIED/ AS GLUCURONIDES OR SULFATES. In rats linuron is metabolized by demethoxylation followed by hydroxylation of the benzene ring. Major urinary metabolites are urea derivatives; no unchanged linuron could be demonstrated. Only trace amounts of 3,4-dichloroaniline were found. If metabolism to dichloroaniline is major pathway in humans, ... methemoglobinemia should be anticipated after toxic doses. For more Metabolism/Metabolites (Complete) data for LINURON (9 total), please visit the HSDB record page. |
---|---|
毒性/毒理 (Toxicokinetics/TK) |
Toxicity Summary
Linuron is a weak competitive inhibitor of androgen receptor binding and it inhibits androgen-induced gene expression in vitro. This may partially contribute to the malformations of androgen-dependent tissues in male rats. (A9961) Toxicity Data LC50 (rat) = 48 mg/m3/4h Non-Human Toxicity Values LD50 Rabbit percutaneous greater than 5000 mg ai (as 50% wettable powder)/kg LD50 Rat female oral 4000 mg/kg in starch mucilage /Technical linuron/ LC50 Rat inhalation >4.06 mg/l air/4 hr LD50 Rabbit oral 2250 mg/kg For more Non-Human Toxicity Values (Complete) data for LINURON (11 total), please visit the HSDB record page. |
参考文献 |
|
其他信息 |
Linuron can cause developmental toxicity according to The Environmental Protection Agency (EPA).
Linuron appears as colorless crystals. Non corrosive. Used as an herbicide. Linuron is a member of the class of phenylureas that is N-methyl urea substituted by a methoxy group at position 1 and a 3,4-dichlorophenyl group at position 3. It has a role as a xenobiotic, an environmental contaminant, a herbicide and an agrochemical. It is a dichlorobenzene and a member of phenylureas. It is functionally related to a N-methyl urea. Linuron is an herbicide for the pre- and post-emergence control of annual grass and broad-leaved weeds using selective and systemic action with contact and residual action. It is known to inhibit photosynthesis (photosystem II). A selective pre- and post-emergence herbicide. (From Merck Index, 11th ed) Mechanism of Action Inhibits photosynthesis. |
分子式 |
C9H10CL2N2O2
|
---|---|
分子量 |
249.09
|
精确质量 |
248.011
|
CAS号 |
330-55-2
|
相关CAS号 |
Linuron-d6;1219804-76-8
|
PubChem CID |
9502
|
外观&性状 |
White to off-white solid powder
|
密度 |
1.3±0.1 g/cm3
|
沸点 |
361.7±52.0 °C at 760 mmHg
|
熔点 |
93-94°C
|
闪点 |
172.6±30.7 °C
|
蒸汽压 |
0.0±0.9 mmHg at 25°C
|
折射率 |
1.556
|
LogP |
3.33
|
tPSA |
41.57
|
氢键供体(HBD)数目 |
1
|
氢键受体(HBA)数目 |
2
|
可旋转键数目(RBC) |
2
|
重原子数目 |
15
|
分子复杂度/Complexity |
228
|
定义原子立体中心数目 |
0
|
InChi Key |
XKJMBINCVNINCA-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C9H10Cl2N2O2/c1-13(15-2)9(14)12-6-3-4-7(10)8(11)5-6/h3-5H,1-2H3,(H,12,14)
|
化学名 |
Urea, 3-(3,4-dichlorophenyl)-1-methoxy-1-methyl-
|
别名 |
Garnitan Herbicide 326Linuron
|
HS Tariff Code |
2934.99.9001
|
存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
溶解度 (体外实验) |
DMSO : ~100 mg/mL (~401.46 mM)
|
---|---|
溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (10.04 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (10.04 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液添加到 900 μL 玉米油中并混合均匀。 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 4.0146 mL | 20.0731 mL | 40.1461 mL | |
5 mM | 0.8029 mL | 4.0146 mL | 8.0292 mL | |
10 mM | 0.4015 mL | 2.0073 mL | 4.0146 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。