PF-06882961
- Product Name
- PF-06882961
- CAS No.
- 2230198-02-2
- Chemical Name
- PF-06882961
- Synonyms
- (S)-2-((4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid;PF-06882961;PF 06882961,PF06882961;Danuglipron (PF-06882961);PF-06882961;PF 06882961;PF06882961;2-[[4-[6-[(4-CYANO-2-FLUOROPHENYL)METHOXY]PYRIDIN-2-YL]PIPERIDIN-1-YL]METHYL]-3-[[(2S)-OXETAN-2-YL]M;2-[[4-[6-[(4-cyano-2-fluorophenyl)methoxy]-2-pyridinyl]-1-piperidinyl]methyl]-1-[(2S)-2-oxetanylmethyl;(S)-2-[[4-[6-[(4-Cyano-2-fluorobenzyl)oxy]-2-pyridyl]-1-piperidyl]methyl]-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic Acid;2-[[4-[6-[(4-Cyano-2-fluorophenyl)methoxy]-2-pyridinyl]-1-piperidinyl]methyl]-1-[(2S)-2-oxetanylmethyl]-1H-benzimidazole-6-carboxylic acid;1H-Benzimidazole-6-carboxylic acid, 2-[[4-[6-[(4-cyano-2-fluorophenyl)methoxy]-2-pyridinyl]-1-piperidinyl]methyl]-1-[(2S)-2-oxetanylmethyl]-
- CBNumber
- CB34664137
- Molecular Formula
- C31H30FN5O4
- Formula Weight
- 555.6
- MOL File
- 2230198-02-2.mol
PF-06882961 Property
- Boiling point:
- 782.6±60.0 °C(Predicted)
- Density
- 1.39±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:10.0(Max Conc. mg/mL);18.0(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);179.98(Max Conc. mM) - form
- Solid powder
- pka
- 3.41±0.30(Predicted)
- color
- Off-white to light yellow
- InChIKey
- HYBAKUMPISVZQP-DEOSSOPVSA-N
- SMILES
- C1(CN2CCC(C3=NC(OCC4=CC=C(C#N)C=C4F)=CC=C3)CC2)N(C[C@@H]2CCO2)C2=CC(C(O)=O)=CC=C2N=1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- DC26147
- Product name
- PF-06882961
- Purity
- >98%
- Packaging
- 250mg
- Price
- $2400
- Updated
- 2021/12/16
- Product number
- DC26147
- Product name
- PF-06882961
- Purity
- >98%
- Packaging
- 1g
- Price
- $4800
- Updated
- 2021/12/16
PF-06882961 Chemical Properties,Usage,Production
Uses
PF-06882961 is a potent, orally bioavailable glucagon-like peptide-1 receptor agonist (GLP-1R) agonist. It has blood glucose lowering and weight loss properties and is used to treat type 2 diabetes (T2D) and obesity.
in vitro
For example, a methylene-linked oxetane increased potency ~100-fold relative to the methyl substituent of 5, leading to the
identification of PF-06882961, which is a full agonist (EC50 = 13 nM) in the CS cAMP assay. PF-06882961 also
incorporates a nitrile replacement for the chloride in the benzyl ether region, which served to reduce CLint in HLM as well as in
human hepatocytes.
Reference: J Med Chem. 2022 Jun 23;65(12):8208-8226. https://pubmed.ncbi.nlm.nih.gov/35647711/
in vivo
Intravenous infusion of PF-06882961 during the IVGTT led to an increase in insulin secretion and the rate of glucose disappearance
(K-value). Enhancement of glucose-stimulated insulin secretion by PF-06882961 was concentration-dependent and was
also observed following oral dosing with similar efficacy when compared to administration by IV infusion. Once-daily
administration of PF-06882961 for 2 days also inhibited food intake compared to vehicle-treated monkeys.
Reference: J Med Chem. 2022 Jun 23;65(12):8208-8226. https://pubmed.ncbi.nlm.nih.gov/35647711/
target
PF-06882961, a non-peptide agonist, activates the canonical G protein signaling activity only in the Glucagon-like peptide-1 (GLP-1) receptor with Trp33ECD.
PF-06882961 Preparation Products And Raw materials
Raw materials
Preparation Products
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