规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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靶点 |
USP25(IC50= 0.7 μM);USP28(IC50= 0.6 μM)
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体内研究 (In Vivo) |
USP25/28 抑制剂 AZ1(AZ1;40 mg/kg;强饲法;每天;持续 7 天)可预防葡聚糖硫酸钠 (DSS) 引起的腹泻和体重减轻以及结肠缩短受损[1]。
结肠USP25/28 抑制剂 AZ1(20 mg/kg/天;灌胃;第 1、3 和 6 周每周 6 次)治疗显着减少肿瘤数量。肿瘤表现出 SOCS3 水平升高、pSTAT3 水平降低以及 Wnt 相关基因表达。 AZ1 灌胃对于治疗 Il10-/- 小鼠自发性结肠炎或 Usp25-/- 小鼠 DSS 诱导的结肠炎无效[1]。 USP25/28 抑制剂 AZ1(20 mg/kg/天;灌胃;每次13-20 周 3 天)可延长 AOM/Vil-Cre;Trp53fl/fl (VP) 小鼠的存活时间,并显着抑制结肠肿瘤发生。在 USP25 背景缺陷的情况下,AZ1 治疗对肿瘤发生几乎没有影响[1]。 |
动物实验 |
Animal Model: Male Usp25+/+ and Usp25-/- mice aged 12 weeks[1]
Dosage: 40 mg/kg Administration: Gavage; daily; for 7 days Result: In comparison to control mice, the colons of Usp25-/-mice showed increased expression of proinflammatory cytokines and antibacterial peptides, and they were shielded from the weight loss and diarrhea caused by dextran sulfate sodium (DSS). They also showed impaired colon shortening. |
参考文献 |
分子式 |
C17H16BRF4NO2
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分子量 |
422.22
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精确质量 |
421.0301
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CAS号 |
2165322-94-9
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相关CAS号 |
2165322-94-9
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SMILES |
C1=CC(=C(C=C1COC2=C(C=C(C=C2)Br)CNCCO)C(F)(F)F)F
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InChi Key |
ITHSFXDGKQYOED-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C17H16BrF4NO2/c18-13-2-4-16(12(8-13)9-23-5-6-24)25-10-11-1-3-15(19)14(7-11)17(20,21)22/h1-4,7-8,23-24H,5-6,9-10H2
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化学名 |
2-(5-Bromo-2-(4-fluoro-3-(trifluoromethyl)benzyloxy)benzylamino)ethanol
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别名 |
AZ1 AZ-1 AZ 1 AZ1
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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)
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溶解度 (体外) |
DMSO : 84~250 mg/mL ( 198.95~592.12 mM )
Ethanol : ~84 mg/mL |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.93 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 20.8 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: 2.08 mg/mL (4.93 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.93 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 | 2.3684 mL | 11.8422 mL | 23.6843 mL | |
5 mM | 0.4737 mL | 2.3684 mL | 4.7369 mL | |
10 mM | 0.2368 mL | 1.1842 mL | 2.3684 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) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00940589 | Completed | Drug: Circadin Drug: Placebo |
Alzheimer's Disease Sleep Disorder |
Neurim Pharmaceuticals Ltd. | September 2009 | Phase 2 |