CID16020046

Catalog No.S8694 Batch:S869401

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

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

4.25mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. 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

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.

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.

References

Selleck's CID16020046 has been cited by 1 publication

Cannabidiol and positive effects on object recognition memory in an in vivo model of Fragile X Syndrome: Obligatory role of hippocampal GPR55 receptors [ Pharmacol Res, 2024, 203:107176]	PubMed: 38583687

Cannabidiol and positive effects on object recognition memory in an in vivo model of Fragile X Syndrome: Obligatory role of hippocampal GPR55 receptors [ Pharmacol Res, 2024, 203:107176]

PubMed: 38583687

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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.

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