C16 acid-I-{Lys(C10 diacid)}-KQELRRIGDEF
C16 acid-I-{Lys (C10 diacid)}-KQELRRIGDEF is a cell-permeable and internalizable PTPN1/2 inhibitor, with IC50 values of 107.6 nM and 3375 nM, respectively. C16 acid-I-{Lys (C10 diacid)}-KQELRRIGDEF restores insulin signaling in HepG2 cells. C16 acid-I-{Lys (C10 diacid)}-KQELRRIGDEF achieves glycemic control in db/db diabetic mice. C16 acid-I-{Lys (C10 diacid)}-KQELRRIGDEF can be used in the research of type 2 diabetes.
For research use only. We do not sell to patients.
- Formula: C94H160N20O24
- Molecular Weight:1954.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Fluorescein-labeled Lys9-Flu-D6 (Compound D6) (5 μM; 6-24 h) can penetrate the cell membrane of HepG2 cells, accumulate near the nucleus, and colocalize with ER[1].
Compound D6 (5-20 μM; 24 h) enhances glucose uptake in insulin-resistant HepG2 cells in the 2-NBDG uptake assay[1].
Compound D6 (5-10 μM; 24 h) restores the insulin signaling pathway in HepG2 cells by upregulating the levels of p-IR-β and p-AKT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:5, 10 μM
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Incubation Time:24 h
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Result:Significantly increased levels of both p-IR-β and p-AKT compared to the insulin-resistant model group.
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Cell Line:HepG2 cells
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Concentration:5 μM
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Incubation Time:6, 12, 24 h
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Result:Could penetrate the cell membrane and persist inside the cell for more than 24 hours, accumulating a large amount of intracellular green fluorescence (FAM-labeled peptide) near the cell nucleus.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | Tmax |
|---|---|---|---|---|---|
| Rat[1] | 0.2 mg/kg | s.c. | >200 h | 444.2 ng/mL | 24 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/Ks db/db mice (female, 8-9 weeks old, type 2 diabetes mellitus model)[1]
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Dosage:0.2 mg/kg; 0.4 mg/kg
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Administration:s.c.; once weekly; 8 weeks
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Result:Significantly reduced blood glucose levels, and the hypoglycemic effect is sustained and stable.
Exhibited a long-lasting anti-hyperglycemic effect and duration of action.
Restored circulating glucose levels.
Decreased plasma insulin and C-peptide concentrations to 0.4 mg/kg.
Slightly increased p-Akt and p-STAT3 levels.
Chemical Information
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Molecular Weight 1954.40
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Formula C94H160N20O24
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Sequence
C16 acid-Ile-{Lys(C10 diacid)}-Lys-Gln-Glu-Leu-Arg-Arg-Ile-Gly-Asp-Glu-Phe
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Sequence Shortening
C16 acid-I-{Lys(C10 diacid)}-KQELRRIGDEF
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
C16 acid-I-{Lys(C10 diacid)}-KQELRRIGDEF Related Classifications
HY-P11604 Related Classifications
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