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
- Molecular Weight:
- 555.6
- MDL Number:
- MFCD32661373
- MOL File:
- 2230198-02-2.mol
| 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) |
| 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 |
| FDA UNII | DN9IUI24GP |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
PF-06882961 Chemical Properties,Uses,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
PF-06882961 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Nanjing Bicbiotechnology Co., Ltd | +86-2552131256 +86-18251840740 | sales@bicbiotech.com | China | 6000 | 58 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21691 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 | figo.gao@foxmail.com | China | 6992 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| NINGBOBENKANGJS PHARMTECHCO., LTD | +8615990591583 15990591583 | CHINA | 2029 | 58 | |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Shanxi Tihondan Pharmaceutical Technology Co., Ltd | +8618235132063 | sales@tihondan.com | China | 3716 | 58 |
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