CID16020046

Catalog No.S8694 Batch:S869401

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Technical Data

Formula

C25H19N3O4
Molecular Weight 425.44 CAS No. 834903-43-4
Solubility (25°C)* In vitro DMSO 85 mg/mL (199.79 mM)
Water Insoluble
Ethanol Insoluble
* <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 CID16020046 (C390-0219) is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
Targets
GPR55 [2]
(in yeast)
0.15 μM
In vitro

In yeast cells expressing human GPR55, CID16020046 antagonized agonist-induced receptor activation. In human embryonic kidney (HEK293) cells stably expressing human GPR55, the compound behaved as an antagonist on LPI-mediated Ca2+ release and extracellular signal-regulated kinases activation, but not in HEK293 cells expressing cannabinoid receptor 1 or 2 (CB1 or CB2). CID16020046 concentration dependently inhibited lysophosphatidylinositol (LPI)-induced activation of nuclear factor of activated T-cells (NFAT), nuclear factor κ of activated B cells (NF-κB) and serum response element, translocation of NFAT and NF-κB, and GPR55 internalization[2].
In vivo

CID16020046 improves inflammation in models of intestinal inflammation and reduces proinflammatory cytokines. CID16020046 does not change the locomotor and anxiety behavior of healthy mice[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    J774A.1 cells

  • Concentrations

    1, 5 and 10 μM

  • Incubation Time

    30 min

  • Method

    2 × 106 cells were transferred into 500 μL PBS and preincubated for 30 mins with 1, 5, and 10 μM CID16020046 or vehicle (DMSO). Cells were then stimulated with 1 nM of monocyte chemotactic protein 1 (MCP-1) for another 30 mins at 37°C. Alexa Fluor 647 anti-mouse CD11b was added 15 min before the end of the incubation time. After adding the fixative solution, cells were measured on a FACSCalibur flow cytometer. Experiments were performed in triplicates and data were expressed as percentage change to the vehicle treatment.
Animal Study:

[1]
  • Animal Models

    C57BL/6 mice

  • Dosages

    20 mg/kg

  • Administration

    s.c.

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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.