C16 acid-I-{Lys(C10 diacid)}-KQELRRIGDEF

Cat. No.: HY-P11604: Ficha de datos Instrucciones de manejo
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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.

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C16 acid-I-{Lys(C10 diacid)}-KQELRRIGDEF Estructura química

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Descripciòn

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.

Western Blot Analysis^[1]

Cell Line:	HepG2 cells
Concentration:	5, 10 μM
Incubation Time:	24 h
Result:	Significantly increased levels of both p-IR-β and p-AKT compared to the insulin-resistant model group.

Immunofluorescence^[1]

Cell Line:	HepG2 cells
Concentration:	5 μM
Incubation Time:	6, 12, 24 h
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	T_1/2	C_max	T_max
Rat^[1]	0.2 mg/kg	s.c.	>200 h	444.2 ng/mL	24 h

In Vivo

Compound D6 (0.2-0.4 mg/kg; subcutaneous injection; once weekly; for 8 consecutive weeks) exerts sustained hypoglycemic effects and improves insulin sensitivity in db/db diabetic model mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/Ks db/db mice (female, 8-9 weeks old, type 2 diabetes mellitus model)^[1]
Dosage:	0.2 mg/kg; 0.4 mg/kg
Administration:	s.c.; once weekly; 8 weeks
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.

Peso molecular

1954.40

Fòrmula

C₉₄H₁₆₀N₂₀O₂₄

Sequence

C16 acid-Ile-{Lys(C10 diacid)}-Lys-Gln-Glu-Leu-Arg-Arg-Ile-Gly-Asp-Glu-Phe

Sequence Shortening

C16 acid-I-{Lys(C10 diacid)}-KQELRRIGDEF

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Zhang C, et al. Dual Conjugation of Long- and Medium-Chain Fatty Acids to BimBH3 Peptide Yields Ultra Long-Acting Inhibitors of Intracellular PTPN1/2. J Med Chem. 2025;68(11):11174-11187. [Content Brief]