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PTP1B/AKR1B1-IN-2

Cat. No. M42549
PTP1B/AKR1B1-IN-2 Structure
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Quality Control & Documentation
Biological Activity

PTP1B/AKR1B1-IN-2 is a dual PTP1B/AKR1B1 inhibitor (IC50s: 3.2 and 2.1 μM, Kis: 4.0 and 0.9μM).

Chemical Information
Molecular Weight 441.56
Formula C23H23NO4S2
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jiupeng Zhou et al. Medicine (Baltimore). The role of PTP1B (PTPN1) in the prognosis of solid tumors: A meta-analysis

[2] Pei-Jie Chen et al. Curr Cancer Drug Targets. Protein Tyrosine Phosphatase 1B (PTP1B): Insights into its New Implications in Tumorigenesis

[3] Maryam Teimouri et al. J Physiol Biochem. The role of protein tyrosine phosphatase 1B (PTP1B) in the pathogenesis of type 2 diabetes mellitus and its complications

[4] Florian Wiede et al. Cancer Discov. PTP1B Is an Intracellular Checkpoint that Limits T-cell and CAR T-cell Antitumor Immunity

[5] Akhilesh Kumar Tamrakar et al. Expert Opin Ther Pat. PTP1B inhibitors for type 2 diabetes treatment: a patent review (2011 - 2014)

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  Catalog
Abmole Inhibitor Catalog




Keywords: PTP1B/AKR1B1-IN-2 supplier, Phosphatase, inhibitors, activators


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