Home Metabolism phosphatase inhibitor BVT-948

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BVT-948 phosphatase inhibitor

Cat.No.S9829

BVT 948 is a irreversible, noncompetitive and cell-permeable protein tyrosine phosphatase（PTP） inhibitor with IC50s of 0.9 μM, 1.7 μM, 0.09 μM, 1.5 μM and 0.7 μM for PTP1B, TCPTP, SHP-2, LAR and YopH respectively.
BVT-948 phosphatase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 241.24

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Quality Control

Batch: S982901 DMSO]48 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.77%
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99.77

Solubility

In vitro
Batch:

DMSO : 48 mg/mL (198.97 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 241.24 Formula

C14H11NO3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 39674-97-0 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1(C)C(=O)N=C2C3=CC=CC=C3C(=O)C(=C12)O

Mechanism of Action

Targets/IC50/Ki
SHP-2
(Cell-free assay)
0.09 μM
YopH
(Cell-free assay)
0.7 μM
PTP1B
(Cell-free assay)
0.9 μM
LAR
(Cell-free assay)
1.5 μM
TCPTP
(Cell-free assay)
1.7 μM
In vitro

In L6 myotubes, PTP1B is oxidized further to the irreversible sulfinic and sulfonic forms with BVT.948. BVT.948 is able to increase tyrosine phosphorylation of cellular proteins, including the insulin receptor. BVT.948 inhibits several other PTPs tested and also was efficient at inhibiting several cytochrome P450 (P450) isoforms.
In vivo

BVT.948 enhances insulin tolerance tests in ob/ob mice, therefore apparently enhancing insulin sensitivity. BVT.948 can significantly enhance glucose clearance from the blood stream in response to insulin.

References

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