7-Ethoxyresorufin
(Synonyms: 乙氧基试卤灵,Resorufin ethyl ether) 目录号 : GC13784
A fluorogenic substrate for, and inhibitor of, CYP1A1
Cas No.:5725-91-7
Sample solution is provided at 25 µL, 10mM.
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Cytochrome P450, family 1, subfamily A, polypeptide 1 is a protein that is encoded by human CYP1A1 gene. The protein is a member of the cytochrome P450 superfamily of enzymes. CYP1A1 is involved in phase I xenobiotic and drug metabolism. CYP1A1 is inhibited by fluoroquinolones and macrolides and induced by aromatic hydrocarbons. 7-Ethoxyresorufin is a specific subtrate of CYP1A.
In vitro: 7-Ethoxyresorufin (2-10 microM), a substrate for cytochrome P450, which binds to the heme moiety of the enzyme, reduced responses to acetylcholine concentration-dependently but not the other agonists indicating an effect on nitric oxide synthesis although neither affected the conversion of L-arginine to L-citrulline [1].
In vivo: Activities of CYP1A (7-ethoxyresorufin) in the liver was determined for comparative purposes. In mice, LPS depressed CYP2A5 at low doses but not at doses that increased pro-inflammatory cytokines and NO serum levels, and depressed CYP1A activity. Blockade of proinflammatory cytokines extended down-regulation of CYP2A5 while not affecting LPS-induced depression of CYP1A [2].
Clinical trial: Cytochrome P-450 enzyme activities of 7-ethoxyresorufin O-deethylase (ERDE) was measured in human liver needle biopsy samples from smokers and non-smokers. ERDE activity was significantly elevated in the livers of cigarette smokers. No correlation was observed between plasma cotinine concentration and ERDE activity [3].
References:
[1] Oyekan AO, McGiff JC, Rosencrantz-Weiss P, Quilley J. Relaxant responses of rabbit aorta: influence of cytochrome P450 inhibitors. J Pharmacol Exp Ther. 1994 Jan;268(1):262-9.
[2] De-Oliveira AC, Poça KS, Totino PR, Paumgartten FJ. Modulation of cytochrome P450 2A5 activity by lipopolysaccharide: low-dose effects and non-monotonic dose-response relationship. PLoS One. 2015 Jan 30;10(1):e0117842.
[3] Pelkonen O, Pasanen M, Kuha H, Gachalyi B, Kairaluoma M, Sotaniemi EA, Park SS, Friedman FK, Gelboin HV. The effect of cigarette smoking on 7-ethoxyresorufin O-deethylase and other monooxygenase activities in human liver: analyses with monoclonal antibodies. Br J Clin Pharmacol. 1986 Aug;22(2):125-34.
| Cas No. | 5725-91-7 | SDF | |
| 别名 | 乙氧基试卤灵,Resorufin ethyl ether | ||
| 化学名 | 7-ethoxy-3H-phenoxazin-3-one | ||
| Canonical SMILES | CCOC1=CC2=C(N=C3C=CC(C=C3O2)=O)C=C1 | ||
| 分子式 | C14H11NO3 | 分子量 | 241.24 |
| 溶解度 | DMF : 2 mg/mL (8.29 mM; ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.1452 mL | 20.7262 mL | 41.4525 mL |
| 5 mM | 0.829 mL | 4.1452 mL | 8.2905 mL |
| 10 mM | 0.4145 mL | 2.0726 mL | 4.1452 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet