规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
靶点 |
DREADD; Dopamine receptor; muscarinic M4 receptor
|
---|---|
体外研究 (In Vitro) |
氯氮平 N-氧化物 (CNO) 可以在 DREADD 激活所需的浓度下与非 DREADD 吸收结合,并经过逆转解读母体化合物氯平,氯氮平是一种非典型抗精神病药物,可作用于多种药理靶点并产生多种生理和行为影响[2]。
|
体内研究 (In Vivo) |
在向小鼠单次腹膜内 (ip) 注射钛氧化物细胞氮平 (1 mg/kg) 后,钛氧化物细胞氮平 (CNO) 神经细胞水平在 15 分钟内达到高峰,2 小时后非常低。 CNO在小鼠体内的胚胎半期衰退,但对表达DREADD的实验动物进行迅速处理后所描述的生物学效应通常要长分裂(6-10小时)[1]。
|
动物实验 |
standard laboratory rats and mice
1.0, 3.2, 10.0 mg/kg for rats; 1.25, 2.5, 5.0, 10.0, 20.0 mg/kg for mice i.p. |
参考文献 |
分子式 |
C18H19CLN4O
|
---|---|
分子量 |
342.82266
|
精确质量 |
342.12
|
元素分析 |
C, 63.06; H, 5.59; Cl, 10.34; N, 16.34; O, 4.67
|
CAS号 |
34233-69-7
|
相关CAS号 |
Clozapine; 5786-21-0; Clozapine N-oxide dihydrochloride; 2250025-93-3; 54241-01-9 (HCl); 34233-69-7 (N-oxide); 5786-21-0
|
外观&性状 |
Solid powder
|
SMILES |
C[N+]1(CCN(CC1)C2=NC3=C(C=CC(=C3)Cl)NC4=CC=CC=C42)[O-]
|
InChi Key |
OGUCZBIQSYYWEF-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C18H19ClN4O/c1-23(24)10-8-22(9-11-23)18-14-4-2-3-5-15(14)20-16-7-6-13(19)12-17(16)21-18/h2-7,12,20H,8-11H2,1H3
|
化学名 |
3-chloro-6-(4-methyl-4-oxidopiperazin-4-ium-1-yl)-11H-benzo[b][1,4]benzodiazepine
|
别名 |
Clozapine N-oxide
|
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) |
DMSO: 68~100 mg/mL (198.4~291.7 mM)
Water: ~68 mg/mL Ethanol: ~8 mg/mL |
---|---|
溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 0.5 mg/mL (1.46 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 0.5 mg/mL (1.46 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: 5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 3.4mg/ml (9.92mM) Solubility in Formulation 7: 2.44 mg/mL (7.12 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). 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 | 2.9170 mL | 14.5849 mL | 29.1698 mL | |
5 mM | 0.5834 mL | 2.9170 mL | 5.8340 mL | |
10 mM | 0.2917 mL | 1.4585 mL | 2.9170 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) 。
Oxidation of clozapine to clozapine N-oxide (CNO) using Oxone. MethodsX . 2018 Mar 23:5:257-267. td> |
ORTEP representation of the molecular structure of CNO. MethodsX . 2018 Mar 23:5:257-267. td> |
CNO produces clozapine-like interoceptive stimulus effects in standard laboratory rats and mice. Sci Rep . 2018 Mar 1;8(1):3840. td> |
CNO is converted to clozapine in standard laboratory rats and mice. Sci Rep . 2018 Mar 1;8(1):3840. td> |
CNO produces clozapine-like interoceptive stimulus effects in standard laboratory rats and mice. Sci Rep . 2018 Mar 1;8(1):3840. td> |
CNO is converted to clozapine in standard laboratory rats and mice. Sci Rep . 2018 Mar 1;8(1):3840. td> |