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编 号:F475834
分子式:C35H42N2O11
分子量:666.71
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
Syrosingopine (Su 3118) is an orally active lactate transporters (MCT1/MCT4) dual inhibitor, which can reduce glycolysis and induce synthetic lethality in cancer cells when combine with metformin. Syrosingopine shows anti-hypertensive activity by depleting peripheral stores of norepinephrine.

体内研究:
Syrosingopine (5 mg/kg;皮下注射;一次) 表现出抗高血压活性,该活性与通过耗尽外周去甲肾上腺素储存进行神经节阻滞后的结果一样低。Animal Model:Spontaneously hypertensive rats (SHR) (2 to 17-month-age).
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.

体外研究:
Syrosingopine (10 μM;1、3、4 小时) 在 1 小时后引起细胞内乳酸积累,并在 4 小时达到峰值,从而导致 HeLa 细胞内酸化。 Syrosingopine (10 μM;1、2 小时) 通过分别抑制 MCT1-KO 和 MCT4-KO HAP1 细胞中的 MCT4 和 MCT1 来减缓乳酸流出。 Syrosingopine (10-100 μM)-二甲双胍组合通过抑制 HAP1 MCT1-KO 细胞中乳酸的转运诱导合成致死性。
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