Syrosingopine_product_DataBase

Bioactivity	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[1][2].
Target	MCT1 and MCT4
Invitro	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:
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:
Name	Syrosingopine
CAS	84-36-6
Formula	C35H42N2O11
Molar Mass	666.71
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Reference	[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.

PeptideDB

Syrosingopine

CAS: 84-36-6 F: C35H42N2O11 W: 666.71