1. GPCR/G Protein
  2. Glucagon Receptor
  3. PF-06882961

PF-06882961 

Cat. No.: HY-125824 Purity: 98.50%
Handling Instructions

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R).

For research use only. We do not sell to patients.

PF-06882961 Chemical Structure

PF-06882961 Chemical Structure

CAS No. : 2230198-02-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 428 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R)[1][2].

IC50 & Target

GLP-1R[1][2]

In Vivo

PF-06882961 (3-240 mg per day) shows mild to moderate damage to the heart, moderate to severe effects on the thymus gland (which helps with managing infection), mild to moderate stomach ulcers at the highest dose level given in the rat[3].
PF-06882961 (3-240 mg per day) results one death in an earlier 2-week monkey study at the highest PF-06882961 dose given in that study. No deaths are seen in the 6-week monkey study or any other monkey studies at any of the doses given[3].

Animal Model: 4-week rat[3]
Dosage: 3 mg, 10 mg, 30 mg, 60 mg, 120 mg, and 240 mg per day
Administration:
Result: Mild to moderate damage to the heart, moderate to severe effects on the thymus gland, and mild to moderate stomach ulcers at the highest dose level.
Animal Model: 2-week and 6-week monkeys[3]
Dosage: 3 mg, 10 mg, 30 mg, 60 mg, 120 mg, and 240 mg per day
Administration:
Result: No side effects were observed in the 6-week monkey study. There was one death in an earlier 2-week monkey study at the highest dose. No deaths were seen in the 6-week monkey study or any other monkey studies at any of the doses given.
Molecular Weight

555.60

Formula

C₃₁H₃₀FN₅O₄

CAS No.

2230198-02-2

SMILES

OC(C1=CC=C(N=C(CN2CCC(C3=NC(OCC4=CC=C(C#N)C=C4F)=CC=C3)CC2)N5C[[email protected]]6OCC6)C5=C1)=O

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 : 125 mg/mL (224.98 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (3.91 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (3.91 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (3.91 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.50%

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Keywords:

PF-06882961PF06882961PF 06882961Glucagon ReceptorGCGRorallybioavailableGLP-1RT2DMDiabetesDiseaseInhibitorinhibitorinhibit

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Product name:
PF-06882961
Cat. No.:
HY-125824
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