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| 25mg |
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Purity: ≥98%
Diphenylterazine (DTZ) is a novel bioluminescence agent that showed superior in vitro and in vivo sensitivity over commonly used bioluminescence reporters. As a Red-shifted bioluminescence reporter, it has the potential to be used for biological imaging.
| ln Vitro |
Millimolar concentrations of diphenylterazine have negligible cytotoxic effects [1]. Diphenyltrazine has strong in vivo pharmacokinetics, red-shifted emission, a high quantum yield, and the absence of cofactors needed for light emission. Yeh AH (2023) designed a small and stable protein scaffold from scratch to make the size and shape of the pocket suitable for diphenyltetrazine using the multinuclear transport factor NTF2-like superfamily as the target topology and diphenyltrazine as the target substrate of luciferase. By removing luciferase with a high degree of selectivity, this technique overcomes the limitations of naturally occurring proteins. Although the substrate apex of the de novo designed luciferase is higher, its catalytic efficiency towards diphenyltetrazine (kcat/Km = 106/M/s) is similar to that of natural luciferase [2]. NOTE: To make a 30 mM DTZ stock solution with 5 mM L-ascorbic acid, dissolve 1 mg of DTZ in 88 μL of master mix after first making a premix by dissolving 17.6 mg of L-ascorbic acid in 10 mL of ethanol and 10 mL of 1,2-propanediol [3].
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| ln Vivo |
Background emission is absent when diphenyltetrazine is injected into untransfected BALB/c electrodes. Extended kinetics are shown in the bioluminescence generated by intraperitoneal injection of diphenyltetrazine [1]. The xenograft NU/J tumor model can be used to track the growth of treatment with diphenyltetrazine (0.3 μMol/mouse; 1.13 mg.mL–1/100 μL/mouse) [4].
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| References |
[1]. Yeh HW, et al. Red-shifted luciferase-luciferin pairs for enhanced bioluminescence imaging. Nat Methods. 2017 Oct;14(10):971-974.
[2]. Yeh AH, et al. De novo design of luciferases using deep learning. Nature. 2023 Feb;614(7949):774-780. [3]. Practical Notes for teLuc-DTZ and Antares2-DTZ (updated 07/29/2019). [4]. Hsien-Wei Yeh, et al. ATP-Independent Bioluminescent Reporter Variants To Improve in Vivo Imaging. ACS Chem Biol. 2019 May 17;14(5):959-965 |
| Molecular Formula |
C25H19N3O
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|---|---|
| Molecular Weight |
377.447
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| Exact Mass |
377.1528
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| Elemental Analysis |
C, 79.55; H, 5.07; N, 11.13; O, 4.24
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| CAS # |
344940-63-2
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| Appearance |
Solid powder
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| SMILES |
O=C1C(CC2=CC=CC=C2)=NC3=C(C4=CC=CC=C4)NC(C5=CC=CC=C5)=CN31
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| InChi Key |
HYQVAZNNCBIZSK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19N3O/c29-25-21(16-18-10-4-1-5-11-18)27-24-23(20-14-8-3-9-15-20)26-22(17-28(24)25)19-12-6-2-7-13-19/h1-15,17,26H,16H2
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| Chemical Name |
2-benzyl-6,8-diphenylimidazo[1,2-a]pyrazin-3(7H)-one
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| Synonyms |
DTZ; Diphenylterazine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
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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| Solubility (In Vitro) |
Solubility in DMF : ~11.0 mg/mL (~29.0 mM, with sonication; Note: DMSO can inactivate the activity of Diphenylterazine)
Solubility in EtOH+HCl : ~1 mg/mL (~2.6 mM; with sonication and warming, and adjust pH to 2 with 1M HCl and heat to 80°C;Note: DMSO can inactivate the activity of Diphenylterazine) Solubility in H2O : Insoluble (< 0.1 mg/mL; Note: DMSO can inactivate the activity of Diphenylterazine) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.11 mg/mL (2.94 mM) (saturation unknown) in 10% DMF 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
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 mg/mL (5.30 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6494 mL | 13.2468 mL | 26.4936 mL | |
| 5 mM | 0.5299 mL | 2.6494 mL | 5.2987 mL | |
| 10 mM | 0.2649 mL | 1.3247 mL | 2.6494 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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Reference:Nat Methods. 2017 Oct; 14(10): 971–974. |
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