Danuglipron (Synonyms: PF-06882961)

Name: Danuglipron
Brand: MedChemExpress
SKU: HY-125824
Rating: 5.0 (4 reviews)

Cat. No.: HY-125824 Pureza: 99.85%: Ficha de datos
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Danuglipron (PF-06882961) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. Danuglipron has the potential for type 2 diabetes research.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS : 2230198-02-2

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Revisión del cliente

Based on 4 publication(s) in Google Scholar

Other Forms of Danuglipron:

Danuglipron tromethamine Obtener un presupuesto

4 Publications Citing Use of MCE Danuglipron

Cell Proliferation/Viability Assay

RT-PCR

In Vivo Efficacy Study

: Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]; (A) NRCMs were treated with different concentrations of Danuglipron (PF; 0, 0.05, 0.1, 0.3, 0.9, and 1.2μg/mL) for 24 h, and cell viability was assessed to determine the dose-dependent effects of PF on cardiomyocyte survival. (B) NRCMs were treated with 0.1μg/mL PF for 0, 12, 24, 48, 72, and 96h, followed by the assessment of cell viability at each time point.

: Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]; Neonatal rat cardiomyocytes (NRCMs) were treated with 100 μM PE for 24–48 h to induce hypertrophy, with or without co‐treatment with Danuglipron (PF) at the previously determined optimal concentration of 0.1 μg/mL. Representative immunofluorescence images of NRCMs stained for α-actinin (red) under different treatment conditions: PBS (control), PF alone, PE alone, and PE+PF.

: Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]; Neonatal rat cardiomyocytes (NRCMs) were treated with 100 μM PE for 24–48 h to induce hypertrophy, with or without co‐treatment with Danuglipron (PF) at the previously determined optimal concentration of 0.1 μg/mL. Relative mRNA expression levels of hypertrophy-related markers (ANP, BNP, and β-MHC) in NRCMs under different treatment conditions, as determined by RT-PCR.

: Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]; Danuglipron (PF; 1, 3, 9 mg/kg; po; daily for 8 weeks was initiated 3 days after AB surgery) in C57BL/6 mice using aortic banding (AB) surgery. Representative M-mode echocardiographic images of left ventricular function in different treatment groups.

: Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]; Danuglipron (PF; 1, 3, 9 mg/kg; po; daily for 8 weeks was initiated 3 days after AB surgery) in C57BL/6 mice using aortic banding (AB) surgery revealed that hearts from AB mice were significantly enlarged, with hypertrophic cardiomyocytes compared to the sham group. Representative images of gross morphology of mouse hearts (A), (B) H&E-stained cross-sections of the hearts.

: Danuglipron purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2025 Mar;29(5):e70488. [Abstract]; Danuglipron (PF; 1, 3, 9 mg/kg; po; daily for 8 weeks was initiated 3 days after AB surgery) in C57BL/6 mice using aortic banding (AB) surgery treatment dose‐dependently increased p‐AMPKα levels in AB mice, with the low dose showing the most pronounced effect. Representative western blot images showing the expression of p-AMPKα, AMPKα, and HSP70 in heart tissues from C57BL/6 mice across different treatment groups. GAPDH serves as a loading control.

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Revisión del cliente

Descripciòn

Danuglipron (PF-06882961) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist. Danuglipron has the potential for type 2 diabetes research^[1]^[2].

IC₅₀ & Target

GLP-1R^[1]^[2]

In Vitro

Danuglipron (PF-06882961) shows agonist activities at both the cAMP and βArr pathways. Danuglipron is a full agonist (EC₅₀ of 13 nM) in the CS cAMP assay. Danuglipron is a partial agonist in recruiting βArr2 (EC₅₀ of 490 nM)^[1].

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

In Vivo

Danuglipron (PF-06882961; 10 mg/kg; po; a single dose) reduces blood glucose levels following intraperitoneal glucose tolerance test (IPGTT) in the hGLP-1R mouse model^[2].
Pharmacokinetic Parameters of Danuglipron in Male Wistar rats and Male cynomolgus monkeys^[1].
1.19

Species	Dose (mg/kg)	C_max (ng/mL)	T_max (h)	AUC_0–∞ (ng h/mL)	CL_p (mL/min/kg)	Vd_ss (L/kg)	t_1/2 (h)	Oral F (%)
rat	1.0 (iv)	-	-	296 ± 39.8	57.3 ± 8.68	0.86 ± 0.38	1.13 ± 0.84	-
rat	5.0 (po)	141	0.5	168	-	-	0.63	11
rat	100 (po)	2820	0.75	11900	-	-	2.37	39
monkey	1.0 (iv)	-	-	1240	13.8	0.266	1.89	-
monkey	5.0 (po)	68.7	1.5	303	-	-	6.92	5.0
monkey	100 (po)	1150 ± 715	3.3 ± 2.5	11000 ± 3500	-	-	6.37	9.0

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

Animal Model:	C57BL/6 mice expressing humanized GLP-1R^[2]
Dosage:	10 mg/kg
Administration:	po; a single dose
Result:	Lowered blood glucose levels following IPGTT.

Peso molecular

555.60

Fòrmula

C₃₁H₃₀FN₅O₄

No. CAS

2230198-02-2

Appearance

Solid

Color

White to light yellow

SMILES

FC(C=C(C=C1)C#N)=C1COC2=NC(C(CC3)CCN3CC(N(C4=C5)C[C@@H]6CCO6)=NC4=CC=C5C(O)=O)=CC=C2

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (179.99 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	1.7999 mL	8.9993 mL	17.9986 mL
5 mM	0.3600 mL	1.7999 mL	3.5997 mL
10 mM	0.1800 mL	0.8999 mL	1.7999 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.

Calculadora de molaridad
Calculadora de dilución

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.85%

Select Batch:

Ficha de datos (276 KB) SDS (393 KB)

COA (247 KB) HNMR (206 KB) RP-HPLC (255 KB) LCMS (94 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. David A Griffithm, et al. A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor. J Med Chem. 2022 Jun 23;65(12):8208-8226. [Content Brief]

[2]. W. GUO, et al. Preclinical pharmacology of low molecular weight GLP-1 receptor agonist XW014.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7999 mL	8.9993 mL	17.9986 mL	44.9964 mL
	5 mM	0.3600 mL	1.7999 mL	3.5997 mL	8.9993 mL
	10 mM	0.1800 mL	0.8999 mL	1.7999 mL	4.4996 mL
	15 mM	0.1200 mL	0.6000 mL	1.1999 mL	2.9998 mL
	20 mM	0.0900 mL	0.4500 mL	0.8999 mL	2.2498 mL
	25 mM	0.0720 mL	0.3600 mL	0.7199 mL	1.7999 mL
	30 mM	0.0600 mL	0.3000 mL	0.6000 mL	1.4999 mL
	40 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1249 mL
	50 mM	0.0360 mL	0.1800 mL	0.3600 mL	0.8999 mL
	60 mM	0.0300 mL	0.1500 mL	0.3000 mL	0.7499 mL
	80 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL
	100 mM	0.0180 mL	0.0900 mL	0.1800 mL	0.4500 mL

Danuglipron Related Classifications

Metabolic Disease

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:

Danuglipron2230198-02-2PF-06882961PF06882961PF 06882961GCGRGlucagon ReceptororallybioavailableGLP-1RT2DMDiabetesDiseaseInhibitorinhibitorinhibit

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Danuglipron (Synonyms: PF-06882961)

Revisión del cliente

Other Forms of Danuglipron:

Danuglipron Related Antibodies

4 Publications Citing Use of MCE Danuglipron

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Danuglipron Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Danuglipron Related Classifications

Keywords:

Productos vistos recientemente:

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