Furimazine (PBI 3939)
目录号 : GC32913Furimazine是一种咪唑并吡嗪酮类的发光底物。在哺乳动物细胞中，NanoLuc(Nluc)与Furimazine联用，产生更亮的发光，比带Coelenterazine的Oluc-19高250万倍。
Cas No.:1374040-24-0
Sample solution is provided at 25 µL, 10mM.
Furimazine is an imidazopyrazinone substrate. NanoLuc (Nluc) paired with Furimazine produced 2.5 million-fold brighter luminescence in mammalian cells relative to Oluc-19 with Coelenterazine.
Furimazine is a Coelenterazine analogue.The apparent Km for purified NanoLuc (Nluc) using either Furimazine or Coelenterazine is ~10 μM, while the maximum luminescence (i.e., apparent Vmax) is ~30-fold higher for Furimazine than for native Coelenterazine. Measurement of luminescence intensity from cells expressing Nluc reveals that maximal signal is attained at about 10-20 μM Furimazine[1].
[1]. Hall MP, et al. Engineered luciferase reporter from a deep sea shrimp utilizing a novel imidazopyrazinone substrate. ACS Chem Biol. 2012 Nov 16;7(11):1848-57.
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Kinase experiment: |
Random libraries are generated by error-prone PCR (average of 2-3 mutations per clone). Library 1 (phase 1; template=Oluc-N166R) is screened (4,400 variants) with Coelenterazine. Library 2 (phase 2; template=C1A4E) is screened (4,400 variants) with 11 novel Coelenterazine analogues: 3840, 3841, 3842, 3857, 3880, 3881, 3886, 3887, 3889, 3897, and 3900. The 11 analogues represent substitutions at positions 2, 6, and 8 and are considered to be representative of the entire set of 24 compounds; 2,200 variants are screened with compounds 3896 and 3894. All hits (improved luminescence) are screened again with the remaining Coelenterazine analogues. Library 3 (phase 3; template=C1A4E+Q18L/K33N/F54I/F68Y/L72Q/M75K/I90V) was screened in the context of a mouse Id-X-HaloTag (where X=library) using Coelenterazine and Furimazine. Library screens are performed on a Freedom robotic workstation as follows: induced bacterial cultures (in 96-well microtiter plates) are lysed with a buffer containing 300 mM HEPES pH 8, 200 mM thiourea, 0.3X Passive Lysis Buffer, 0.3 mg/mL lysozyme, and 0.002 units of RQ1 DNase. Assay reagent containing 1 mM CDTA, 150 mM KCl, 10 mM DTT, 0.5% (v/v) Tergitol, and 20 μM substrate is then added to equal volumes of lysate. Samples are measured on a GENios Pro luminometer[1]. |
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References: [1]. Hall MP, et al. Engineered luciferase reporter from a deep sea shrimp utilizing a novel imidazopyrazinone substrate. ACS Chem Biol. 2012 Nov 16;7(11):1848-57. |
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| Cas No. | 1374040-24-0 | SDF | |
| Canonical SMILES | O=C1C(CC2=CC=CO2)=NC3=C(CC4=CC=CC=C4)NC(C5=CC=CC=C5)=CN31 | ||
| 分子式 | C24H19N3O2 | 分子量 | 381.43 |
| 溶解度 | DMSO : ≥ 100 mg/mL (262.17 mM) | 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 | 2.6217 mL | 13.1086 mL | 26.2171 mL |
| 5 mM | 0.5243 mL | 2.6217 mL | 5.2434 mL |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6217 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
