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Syrosingopine MCT inhibitor

Cat.No.S9907

Syrosingopine is a dual MCT1 and MCT4 inhibitor with IC50 values of 2500nM and 40 nM in HAP1 cells, respectively.
Syrosingopine MCT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 666.71

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Quality Control

Batch: Purity: 99.51%
99.51

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (149.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 666.71 Formula

C35H42N2O11

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 84-36-6 -- Storage of Stock Solutions

Synonyms Su-3118 Smiles CCOC(=O)OC1=C(OC)C=C(C=C1OC)C(=O)OC2CC3CN4CCC5=C([NH]C6=C5C=CC(=C6)OC)C4CC3C(C2OC)C(=O)OC

Mechanism of Action

Targets/IC50/Ki
MCT4
(in HAP1 cell)
40 nM
MCT1
(in HAP1 cell)
2500 nM
In vitro

Syrosingopine treatment leads to high intracellular lactate levels and thereby end-product inhibition of lactate dehydrogenase by inhibiting the Lactate Transporters MCT1 and MCT4. The loss of NAD+ regeneration capacity due to combined metformin and syrosingopine treatment results in glycolytic blockade, leading to ATP depletion and cell death. <sup><a class="sref" href="#s_ref">[1]</a></sup>

In vivo

Syrosingopine treatment leads to reduced serum lactate levels significantlyn, and higher intracellular lactate from liver tumor nodules in syrosingopine-treated liver tumor model mice. <sup><a class="sref" href="#s_ref">[1]</a></sup>

References

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