Indole-3-pyruvic acid，色氨酸的酮类类似物，是一种具有口服活性的AHR激动剂。Indole-3-pyruvic acid 具有抗氧化特性，可用于炎症、焦虑的研究。
| 生物活性 | Indole-3-pyruvic acid, a keto analogue of tryptophan, is an orally activeAHRagonist. Indole-3-pyruvic acid has antioxidant properties, and can be used in the research of inflammation, anxiety[1][2][3]. |
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体外研究
(In Vitro) | Indole-3-pyruvic acid (50 and 250 μM, 24 h) activates AHR in HepG2 cells[1].
Indole-3-pyruvic acid (50 μM, 4 days) does not inhibit Th1 cell differentiation but promotes Tr1 differentiation[1].
Indole-3-pyruvic acid (1 mM, 24 h) reduces UVB-induced cytotoxicity in HaCaT cells[1].
Indole-3-pyruvic acid (25 mM, 6 h) reduces the levels of COX-2 in HaCaT cells[2].
RT-PCR[2] | Cell Line: | HaCaT cells | | Concentration: | 5-25 mM | | Incubation Time: | 6 h | | Result: | Inhibited UVB-stimulated mRNA expression of IL-1β, IL-6, and cyclooxygenase 2 (Cox-2). |
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体内研究
(In Vivo) | Indole-3-pyruvic acid (oral administration, fed in MF chow (0.1%) for 5 d) activates AHR in BALB/c mice[1].
Indole-3-pyruvic acid (oral administration, fed in MF chow (0.1%) for 5 wk) abrogates chronic inflammation in a T cell-mediated colitis model[1].
Indole-3-pyruvic acid (100 μM, dose at skin) protects against UVB-induced skin damage in HR-1 hairless mice[2].
Indole-3-pyruvic acid (intraperitoneal injection, 100-200 mg/kg) increases the time spent in the open arms of the elevated plus maze in mice[3].
| Animal Model: | BALB/c mice[1] | | Dosage: | Fed in MF chow.0.1% for 5 d | | Administration: | Oral administration | | Result: | Up-regulated the expression of Cyp1a1 (a biomarker for AHR activation) in the colon. |
| Animal Model: | T cell–mediated colitis model of SCID mice[1] | | Dosage: | Fed in MF chow.0.1% for 5 wk | | Administration: | Oral administration | | Result: | Suppressed diarrhea and improved colon inflammation.
Down-regulated the expression of Th1 and proinflammatory cytokines and upregulated the expression of IL-10 in the colon. |
| Animal Model: | HR-1 Hairless Mice[2] | | Dosage: | 100 μM | | Administration: | Dose at skin | | Result: | Enhanced the epidermal thickness.
Attenuated UVB-induced necrosis observed in upper layer of dermis. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(1230.38 mM;Need ultrasonic) H2O : 20 mg/mL(98.43 mM;ultrasonic and adjust pH to 12 with NaOH) 配制储备液 | 1 mM | 4.9215 mL | 24.6075 mL | 49.2150 mL | | 5 mM | 0.9843 mL | 4.9215 mL | 9.8430 mL | | 10 mM | 0.4922 mL | 2.4608 mL | 4.9215 mL |
*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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 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: ≥ 2.08 mg/mL (10.24 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.24 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (10.24 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (10.24 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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