Theaflavin 3,3′-digallate (TF-3) is a potent Zika virus (ZIKV) protease inhibitor with an IC₅₀ of 2.3 μM. Theaflavin 3,3′-digallat directly binds to ZIKVpro (K_d=8.86 µM) and inhibits ZIKV replication. Theaflavin 3,3′-digallat inhibits the activity of gp41 and NS2B-3 protease and has antiviral activity against HSV and HIV-1^[1]. Theaflavin 3,3′-digallate, the typical pigment in black tea, is a potent antitumor agent^[2].

Theaflavin 3,3′-digallate (TF-3; 6.25, 12.5, 25 μM; 24 hours) markedly reduces viral RNA copy numbers and NS3, U87 MG protein expression in a dose-dependent manner^[1].
Theaflavin 3,3′-digallate inhibits dose-dependently ZIKV replication in Vero E6 cells (EC₅₀=7.65 μM). Theaflavin 3,3′-digallate has minor cytotoxicity up to 40 μM in Vero E6 cells. Theaflavin 3,3′-digallate can inhibit the post-entry events of the ZIKV replication cycle from gene transcription and translation levels^[1].
Theaflavin 3,3′-digallate is generally regarded as the effective component for the inhibitory effects against carcinogenesis without adverse side effects by affecting multiple signal transduction pathways, such as upregulating p53 and p21, inhibiting phosphorylation of the cell survival protein Akt and MAPK pathway, downregulation of NF-κB, shifting the ratio between pro-/antiapoptotic proteins. Theaflavin 3,3′-digallate causes a rapid and sustained decrease in phospho-ERK1/2 and -MEK1/2 protein expression. Theaflavin 3,3′-digallate inhibits HCT116 cell growth with an IC₅₀ of 17.26 μM^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

868.70

C₄₃H₃₂O₂₀

30462-35-2

茶黄素-3,3′-双没食子酸

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

DMSO : 100 mg/mL (115.11 mM; Need ultrasonic)

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (2.88 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [1]. Xiangling Cui, et al. Identification of Theaflavin-3,3′-Digallate as a Novel Zika Virus Protease Inhibitor. Front Pharmacol. 2020 Oct 21;11:514313.

  [2]. Ding Y, et al. Pre-treated theaflavin-3,3′-digallate has a higher inhibitory effect on the HCT116 cell line. Food Nutr Res. 2017 Nov 15;61(1):1400340.