Syrosingopine (Su 3118) 是一种口服有效的乳酸转运蛋白MCT1/MCT4双重抑制剂，可减少糖酵解并可与二甲双胍联合后诱导癌细胞的合成致死性。Syrosingopine 可通过耗损去甲肾上腺素显示抗高血压活性。
| 生物活性 | Syrosingopine (Su 3118) is an orally activelactate transporters(MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality incancercells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine[1][2]. |
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体外研究
(In Vitro) | Syrosingopine (10 μM; 1, 3, 4 hours) causes accumulation of intracellular lactate after 1 hour and peaks at 4 hours, which lead to intracellular acidification in HeLa cells[1].
Syrosingopine (10 μM; 1, 2 hours) slows lactate efflux by inhibiting MCT4 and MCT1 in MCT1-KO and MCT4-KO HAP1 cells, respectively[1].
Syrosingopine (10-100 μM)-metformin combination induces synthetic lethality by inhibiting transport of lactate in HAP1 MCT1-KO cells[1].
Cell Viability Assay[1] | Cell Line: | HeLa, MCT1-KO, MCT4-KO HAP1, HAP1 MCT1-KO | | Concentration: | 10 μM | | Incubation Time: | 1, 2, 3, 4 hours | | Result: | Caused intracellular lactate accumulation and acidification.
Slowed lactate efflux by inhibiting MCT4 and MCT1.
Induced synthetic lethality by inhibiting transport of lactate when combined with metformin. |
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体内研究
(In Vivo) | Syrosingopine (5 mg/kg; s.c.; once) shows anti-hypertensive activity which as low as the result after ganglionic blockade by depleting peripheral stores of norepinephrine[2].
| Animal Model: | Spontaneously hypertensive rats (SHR) (2 to 17-month-age)[2]. | | Dosage: | 5 mg/kg | | Administration: | Subcutaneous injection; once (16 hours before undertaking the study of blood pressure). | | Result: | Showed anti-hypertensive activity by depleting peripheral stores of norepinephrine. |
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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 : 62.5 mg/mL(93.74 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.4999 mL | 7.4995 mL | 14.9990 mL | | 5 mM | 0.3000 mL | 1.4999 mL | 2.9998 mL | | 10 mM | 0.1500 mL | 0.7500 mL | 1.4999 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 (3.12 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.12 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%corn oil Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 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 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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