Danuglipron (PF-06882961)

Catalog No.S9851 Batch:S985101

Technical Data

Formula	C₃₁H₃₀FN₅O₄
Molecular Weight	555.60	CAS No.	2230198-02-2
Solubility (25°C)*	In vitro	Ethanol	100 mg/mL (179.98 mM)
		DMSO	10 mg/mL (17.99 mM)
		Water	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

Danuglipron (PF-06882961), a non-peptide agonist, activates the canonical G protein signaling activity only in the Glucagon-like peptide-1 (GLP-1) receptor with Trp33^ECD.

Targets

GLP-1 receptor ^[1]

In vitro

PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. In contrast, PF-06882961 does not increase cAMP levels in cells expressing the mouse, rat, or rabbit GLP-1R.^[2]

In vivo

PF-06882961 potentiates glucose-stimulated insulin release and reduces food intake in monkeys.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines HEK293 cells Concentrations 1 μM Incubation Time 30 minutes Method HEK293 cells stably expressing hGLP-1R fused to green fluorescent protein (GFP) (400,000 cells per well) are cultured onto 6 well plates for 24 hours and stimulated with PF-06882961 for 30 minutes. An agonist concentration of 1 μM shown to induce maximal internalization is chosen for these studies. In selected wells, cells are washed three times with PBS containing 0.1 % BSA and incubated at 37 °C for an additional 2 hours to assess reversibility of the endocytosis process. Cells are then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS containing 0.1% BSA.
Animal Study:^{^[2]}	Animal Models male cynomolgus monkeys Dosages 1 mg/kg, 5 mg/kg, 100 mg/kg Administration IV, Oral gavage

Cell Assay:^{^[2]}

Cell lines
HEK293 cells
Concentrations
1 μM
Incubation Time
30 minutes
Method
HEK293 cells stably expressing hGLP-1R fused to green fluorescent protein (GFP) (400,000 cells per well) are cultured onto 6 well plates for 24 hours and stimulated with PF-06882961 for 30 minutes. An agonist concentration of 1 μM shown to induce maximal internalization is chosen for these studies. In selected wells, cells are washed three times with PBS containing 0.1 % BSA and incubated at 37 °C for an additional 2 hours to assess reversibility of the endocytosis process. Cells are then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS containing 0.1% BSA.

Animal Study:^{^[2]}

Animal Models
male cynomolgus monkeys
Dosages
1 mg/kg, 5 mg/kg, 100 mg/kg
Administration
IV, Oral gavage

References

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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.