2. GPCR/G Protein Metabolic Enzyme/Protease
  3. GLP Receptor Phosphodiesterase (PDE)
  4. Naperiglipron

Naperiglipron (LY3549492) is an orally active Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research.

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Naperiglipron

Naperiglipron Chemical Structure

CAS No. : 2572566-11-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Naperiglipron Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Naperiglipron (LY3549492) is an orally active Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research[1].

IC50 & Target[1]

PDE10A1

7.43 μM (IC50)

In Vitro

Naperiglipron (Example 2) causes an increase in cAMP levels in HEK293 cells, with its EC50 being 3.97 nM[1].

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

Naperiglipron Related Antibodies
Parmacokinetics
Species Dose Route Vd CL
Monkey1 0.5 mg/kg i.v. 1.1 L/kg 11 mL/min/kg
In Vivo

Naperiglipron (Example 2) (p.o.) exhibits extremely potent hypoglycemic efficacy in mice expressing human GLP-1 receptors, with its ED50 being 0.07 mg/kg[1].

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

580.58

Formula

C33H26F2N4O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(C=C(C=C1)C#N)=C1COC2=NC(C(C(C)=C3)=CC(F)=C3CC4=NC5=CC=C(C(O)=O)C=C5N4C[C@H]6OCC6)=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (86.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7224 mL 8.6121 mL 17.2242 mL
5 mM 0.3445 mL 1.7224 mL 3.4448 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.43%

SDS (252 KB)

COA (250 KB) HNMR (320 KB) LCMS (337 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7224 mL 8.6121 mL 17.2242 mL 43.0604 mL
5 mM 0.3445 mL 1.7224 mL 3.4448 mL 8.6121 mL
10 mM 0.1722 mL 0.8612 mL 1.7224 mL 4.3060 mL
15 mM 0.1148 mL 0.5741 mL 1.1483 mL 2.8707 mL
20 mM 0.0861 mL 0.4306 mL 0.8612 mL 2.1530 mL
25 mM 0.0689 mL 0.3445 mL 0.6890 mL 1.7224 mL
30 mM 0.0574 mL 0.2871 mL 0.5741 mL 1.4353 mL
40 mM 0.0431 mL 0.2153 mL 0.4306 mL 1.0765 mL
50 mM 0.0344 mL 0.1722 mL 0.3445 mL 0.8612 mL
60 mM 0.0287 mL 0.1435 mL 0.2871 mL 0.7177 mL
80 mM 0.0215 mL 0.1077 mL 0.2153 mL 0.5383 mL
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Naperiglipron Related Classifications

Help & FAQs
  • 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.

Keywords:

Naperiglipron2572566-11-9LY3549492LY 3549492LY-3549492GLP ReceptorPhosphodiesterase (PDE)Glucagon-like peptide 1 receptorGLP-1RHEK293 cellsGLP-1R knock-in mouse modelsPDE10A1Type II diabetes mellitusT2DMObesityInhibitorinhibitorinhibit

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