9-Hydroxyellipticine (hydrochloride)
(Synonyms: 9-OH-Ellipticine, NSC 210717) 目录号 : GC45367
An ellipticine derivative with diverse biological activities
Cas No.:52238-35-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
9-Hydroxyellipticine is a derivative of ellipticine with diverse biological activities.1,2,3 It inhibits aroclor-induced activation of aniline hydroxylase, aminopyrine N-demethylase, and 7-ethoxycourmarin O-deethylase in rat liver microsomes (Kis = 3.5, 0.6, and 0.74 μM, respectively).1 9-Hydroxyellipticine inhibits the growth of L1210 murine leukemia cells (IC50 = 3 nM) in vitro and increases survival in an L1210 mouse leukemia model.2,3 It inhibits carrageenan-induced edema and UV-induced erythema in guinea pigs.4
References
1. Lesca, P., Rafidinarivo, E., Lecointe, P., et al. A class of strong inhibitors of microsomal monooxygenases: The ellipticines. Chem. Biol. Interact. 24(2), 189-197 (1979).
2. Monnot, M., Mauffret, O., Simon, V., et al. DNA-drug recognition and effects on topoisomerase II-mediated cytotoxicity. A three-mode binding model for ellipticine derivatives. J. Biol. Chem. 266(3), 1820-1829 (1991).
3. Le Pecq, J.B., Grosse, C., Dat-Xuong, N., et al. Antitumor activity of 9-hydroxyellipticine (NSC 210717) ON L1210 mouse leukemia and the effect of route of injection. Cancer Res. 36(9 pt. 1), 3067-3076 (1976).
4. Cros, J., Thibault, A., and Dat-Xuong, N. Anti-inflammatory effect of hydroxy-9-ellipticine. C. R. Acad. Sci. Hebd. Seances Acad. Sci. D. 281(15), 1139-1142 (1975).
| Cas No. | 52238-35-4 | SDF | |
| 别名 | 9-OH-Ellipticine, NSC 210717 | ||
| Canonical SMILES | CC1=C2C(NC3=C2C=C(O)C=C3)=C(C)C4=C1C=NC=C4.Cl | ||
| 分子式 | C17H14N2O.HCl | 分子量 | 298.8 |
| 溶解度 | DMSO: slightly, heated,Methanol: slightly | 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 | 3.3467 mL | 16.7336 mL | 33.4672 mL |
| 5 mM | 0.6693 mL | 3.3467 mL | 6.6934 mL |
| 10 mM | 0.3347 mL | 1.6734 mL | 3.3467 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。
Metabolism of 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone in mouse lung microsomes and its inhibition by isothiocyanates
Cancer Res 1990 Nov 1;50(21):6817-22.PMID:2208146doi
The tobacco-specific carcinogen 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) induces lung tumors in rats, mice, and hamsters, and metabolic activation is required for the carcinogenicity. 2-Phenethyl isothiocyanate (PEITC), whose precursor gluconasturtiin (a glucosinolate) occurs in cruciferous vegetables, has been found to inhibit carcinogenesis by NNK. The purpose of the study was to investigate the enzymes involved in the metabolism of NNK in lung microsomes and to elucidate the mechanisms of inhibition of NNK metabolism by isothiocyanates. NNK metabolism in lung microsomes (isolated from female A/J mice) resulted in the formation of formaldehyde, 4-hydroxy-1-(3-pyridyl)-1-butanone (keto alcohol), 4-oxo-4-(3-pyridyl)butyric acid (keto acid), 4-(methylnitrosamino)-1-(3-pyridyl-N-oxide)-1-butanone, and 4-(methyl-nitrosamino)-1-(3-pyridyl)-1-butanol, displaying apparent Km values of 5.6, 5.6, 9.2, 4.7, and 2540 microM, respectively. Higher Km values in the formation of formaldehyde and keto alcohol were also observed. When cytochrome P-450 inhibitors [2-(diethylamino)ethyl 2,2-diphenylpentenoate] hydrochloride (100 microM), carbon monoxide (90%), and 9-Hydroxyellipticine (10 microM) were used, NNK metabolism was inhibited by each 70, 100, and 30%, respectively. Methimazole (1 mM), an inhibitor of the flavin-dependent monooxygenase, inhibited the formation of 4-(methyl-nitrosamino)-1-(3-pyridyl-N-oxide)-1-butanone and 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanol by 20%, but had no effect on the formation of keto alcohol. Inhibitory antibodies against cytochromes P-450IIB1 and -2, P-450IA1, and P-450IA2 inhibited the formation of keto alcohol by 25, 15, and 0%, respectively. Administration of PEITC at doses of 5 and 25 mumol/mouse 2 h before sacrifice produced a 40 and 70% decrease in microsomal NNK metabolism, respectively. PEITC and 3-phenylpropyl isothiocyanate exhibited a mixed type of inhibition, and the competitive component of inhibition had apparent Ki values of 90 and 30 nM, respectively. Preincubation of PEITC in the presence of a NADPH-generating system did not result in a further decrease in the formation of NNK metabolites, indicating that the metabolism of PEITC was not required for the inhibition. When a series of isothiocyanates with varying alkyl chain length (phenyl isothiocyanate, benzyl isothiocyanate, PEITC, 3-phenylpropyl isothiocyanate, and 4-phenylbutyl isothiocyanate) were used, the potency of the inhibition increased with the increase in chain length.(ABSTRACT TRUNCATED AT 400 WORDS)