1. Metabolic Enzyme/Protease
  2. MMP
  3. GPLGVRG

GPLGVRG is an MMP13-responsive linker peptide. GPLGVRG can be hydrolyzed by MMP13, which in turn triggers micellar disintegration, loss of amphipathicity, and increases the chondrocyte uptake rate of the related delivery system. GPLGVRG can be used in the research of osteoarthritis.

For research use only. We do not sell to patients.

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GPLGVRG

GPLGVRG Chemical Structure

CAS No. : 915404-04-5

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Description

GPLGVRG is an MMP13-responsive linker peptide. GPLGVRG can be hydrolyzed by MMP13, which in turn triggers micellar disintegration, loss of amphipathicity, and increases the chondrocyte uptake rate of the related delivery system. GPLGVRG can be used in the research of osteoarthritis[1].

IC50 & Target[1]

MMP13

 

In Vitro

The GPLGVRG peptide is selectively cleaved by MMP13 present in IL-1β-stimulated osteoarthritis (OA) chondrocytes, generating a detectable fluorescent signal via FRET substrate cleavage, and this signal is inhibitable by MMP inhibitors[1].

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

In Vivo

Mic-Exo containing GPLGVRG (micelle:exosome mass ratio of 10:1; 250 μM DHA; intra-articular administration; single dose) is an MMP-responsive, cartilage-penetrating delivery system that enables targeted delivery of DHA (HY-B2167) to OA osteocytes and significantly delays the progression of OA in rats[1].

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

Animal Model: Sprague-Dawley (male, 12 weeks old, 300 to 350 g, ACLT+DMM induced knee OA)[1]
Dosage: micelle:exosome protein mass ratio 10:1; 250 μM DHA
Administration: intra-articular; single dose
Result: Reduced Osteoarthritis Research Society International.
Preserved cartilage thickness.
Increased chondrocyte number.
Reduced positive staining for ADAMTS5 to 17.0% versus 79.3% in OA control.
Reduced positive staining for MMP13 to 14.7% versus 72.1% in OA control.
Increased trabecular bone mineral density to 1.4 versus 1.3 in OA control.
Increased trabecular thickness to 0.2 mm versus 0.1 mm in OA control.
Increased bone volume fraction to 45.2% versus 33.9% in OA control.
Penetrated ex vivo rat femoral head cartilage to 74.0 μm versus 32.4 μm for unmodified exosomes at 48 h.
Penetrated ex vivo rat femoral head cartilage to 155.0 μm versus 36.3 μm for unmodified exosomes at 72 h.
Molecular Weight

654.76

Formula

C28H50N10O8

CAS No.
Sequence

Gly-Pro-Leu-Gly-Val-Arg-Gly

Sequence Shortening

GPLGVRG

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Room temperature in continental US; may vary elsewhere.

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

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GPLGVRG
Cat. No.:
HY-P11800
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