HET0016
(Synonyms: N-hydroxy-N'-(4-n-butyl-2-methylphenyl)Formamidine) 目录号 : GC11540
A potent, selective 20-HETE synthase inhibitor
Cas No.:339068-25-6
Sample solution is provided at 25 µL, 10mM.
IC50: 35 nM for 20-HETE formation in rat renal microsomes
HET0016 is an inhibitor of 20-HETE formation.
20-HETE, a major biologically active cytochrome P450 metabolite of arachidonic acid in the kidney and liver, regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation.
In vitro: HET0016 showed a high degree of selectivity in inhibiting the formation of 20-HETE in rat renal microsomes. The IC(50) value averaged 35 nM, whereas the IC(50) value for inhibition of the formation of epoxyeicosatrienoic acids averaged 2800 nM. Moreover, in human renal microsomes, HET0016 could potently inhibit the formation of 20-HETE with an IC(50) value of 8.9 nM. In addition, higher HET0016 concentrations could also inhibit the CYP2C9, CYP2D6 and CYP3A4-catalysed substrates oxidation [1].
In vivo: A previous study generated an improved IV formulation of HET0016 with HPβCD. Administration of a single IV dose led to 7-fold higher levels of HET0016 in plasma and 3.6-fold higher levels in tumor than that in IP route. IV treatment with HPβCD-HET0016 decreased tumor growth, and altered vascular kinetics in early and late treatment groups. Moreover, similar growth inhibition was observed in syngeneic GL261 GBM. In addition, survival studies using patient derived xenografts of GBM811, showed prolonged survival to 26 weeks in animals treated with focal radiation, in combination with HET0016 and TMZ [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Miyata, N. ,Taniguchi, K.,Seki, T., et al. HET0016, a potent and selective inhibitor of 20-HETE synthesizing enzyme. British Journal of Pharmacology 133, 325-329 (2001).
[2] Jain M et al. Intravenous Formulation of HET0016 Decreased Human Glioblastoma Growth and Implicated Survival Benefit in Rat Xenograft Models. Sci Rep. 2017 Jan 31;7:41809.
| Cas No. | 339068-25-6 | SDF | |
| 别名 | N-hydroxy-N'-(4-n-butyl-2-methylphenyl)Formamidine | ||
| 化学名 | N-(4-butyl-2-methylphenyl)-N'-hydroxy-methanimidamide | ||
| Canonical SMILES | CCCCC1=CC=C(/N=C/NO)C(C)=C1 | ||
| 分子式 | C12H18N2O | 分子量 | 206.3 |
| 溶解度 | ≤14mg/ml in ethanol;14mg/ml in DMSO;14mg/ml in dimethyl formamide | 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 | 4.8473 mL | 24.2365 mL | 48.4731 mL |
| 5 mM | 0.9695 mL | 4.8473 mL | 9.6946 mL |
| 10 mM | 0.4847 mL | 2.4237 mL | 4.8473 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
