ADAMTS-5 Inhibitor

Catalog No.E0649 Batch:E064901

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Technical Data

Formula

C16H11ClF3N3OS3

Molecular Weight 449.93 CAS No. 929634-33-3
Solubility (25°C)* In vitro DMSO 90 mg/mL (200.03 mM)
Ethanol 11 mg/mL (24.44 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO Corn oil
4.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description ADAMTS-5 Inhibitor is a potent ADAMTS-5 (aggrecanase-2) inhibitor, with an IC50 of 1.1 µM.
In vitro

ADAMTS-5 Inhibitor protects against IL-1b-induced degradation of proteoglycan and aggrecan in chondrocytes.[2]

In vivo

ADAMTS-5 Inhibitor promotes the in vivo cartilage healing in the osteochondral defect model rats, and prevents the progression of degenerative changes in the anterior cruciate ligament (ACL) model rats.[2]

Protocol (from reference)

Cell Assay:

[2]

  • Cell lines

    Isolated humen chondrocytes

  • Concentrations

    2 μM, 10 μM, 20 μM

  • Incubation Time

    1-3 days

  • Method

    Chondrocytes are suspended at a final concentration of 1×105 cells/well and exposured to ADAMTS-5 Inhibitor for 1-3 days. CCK-8 is added to each well for cell viability assay. Aggrecan is measured by the dye-binding assay. Proteoglycan is shown by Safranin-O staining.

Animal Study:

[2]

  • Animal Models

    Osteoarthritis models SpragueeDawley rats

  • Dosages

    0.12 mg

  • Administration

    i.a.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.