Syrosingopine|84-36-6|-陌孚医药/Medlife

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Syrosingopine

目录号: PL07525 纯度: ≥99%

CAS No. :84-36-6

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中文名称	Syrosingopine
中文别名	昔洛舍平;SY松香GOPINE(RG);羧酯利血平;乙酯利血平;昔可平
英文名称	Syrosingopine
英文别名	Yohimban-16-carboxylicacid, 18-[[4-[(ethoxycarbonyl)oxy]-3,5-dimethoxybenzoyl]oxy]-11,17-dimethoxy-,methyl ester, (3b,16b,17a,18b,20a)-;Syrosingopine;methyl (1R,15S,17R,18R,19S,20S)-17-(4-ethoxycarbonyloxy-3,5-dimethoxybenzoyl)oxy-6,18-dimethoxy-1,3,11,12,14,15,16,17,18,19,20,21-dodecahydroyohimban-19-carboxylate;Elufinesin;Etropres;Isotense;Menatensina;Neoreserpan;Novoserpina;Syringopine;Syrosingopin;Vegaserpina;(3β,16β,17α,18β,20α)-18-[[4-[(Ethoxycarbonyl)oxy]-3,5-dimethoxybenzoyl]oxy]-11,17-dimethoxy-yohimban-16-carboxylic acid methyl ester;Methyl reserpate ester of syringic acid ethyl carbonate;Londomin;Methyl carbethoxysyringoyl reserpate;NSC 77030;Raunova;Seniramin;Singoserp;Siringina;Su 3118;Syringic acid ethyl carbonate ester with methyl reserpate
Cas No.	84-36-6
分子式	C₃₅H₄₂N₂O₁₁
分子量	666.71
包装储存	4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	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 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.
性状	Solid
IC50 & Target[1][2]	MCT1 and MCT4
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. Syrosingopine (10 μM; 1, 2 hours) slows lactate efflux by inhibiting MCT4 and MCT1 in MCT1-KO and MCT4-KO HAP1 cells, respectively. Syrosingopine (10-100 μM)-metformin combination induces synthetic lethality by inhibiting transport of lactate in HAP1 MCT1-KO cells. has not independently confirmed the accuracy of these methods. They are for reference only.
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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)
参考文献	[1]. Benjamin D, et al. Dual Inhibition of the Lactate Transporters MCT1 and MCT4 Is Synthetic Lethal with Metformin due to NAD+ Depletion in Cancer Cells. Cell Rep. 2018 Dec 11;25(11):3047-3058.e4. [2]. Lefèvre-Borg F, et al. Role of the sympathetic nervous system in blood pressure maintenance and in the antihypertensive effects of calcium antagonists in spontaneously hypertensive rats. Hypertension. 1988 Apr;11(4):360-70.

溶解度数据	In Vitro: DMSO : 62.5 mg/mL (93.74 mM; Need ultrasonic)配制储备液

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