Basic Description

Synonyms	PF-06882961 \| Danuglipron \| 2230198-02-2 \| Danuglipron [USAN] \| DN9IUI24GP \| (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 \| 2-[(4-{6-[(4-cyano-2-fluorophenyl)methoxy]pyridin
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	PF-06882961, a non-peptide agonist, activates the canonical G protein signaling activity only in the Glukagon-like peptide-1 (GLP-1) receptor with Trp33^ECD.
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	AGONIST
Mechanism of action	Agonist of GLP-1 receptor
Note	卖完停产，不再备货
Product Description	Information PF-06882961 PF-06882961, a non-peptide agonist, activates the canonical G protein signaling activity only in the Glukagon-like peptide-1 (GLP-1) receptor with Trp33 ECD . Targets GLP-1 receptor In vitro PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. In contrast, PF-06882961 does not increase cAMP levels in cells expressing the mouse, rat, or rabbit GLP-1R. In vivo PF-06882961 potentiates glucose-stimulated insulin release and reduces food intake in monkeys. Cell Research(from reference) Cell lines：HEK293 cells Concentrations：1 μM Incubation Time：30 minutes

Product Properties

ALogP	1.4

Associated Targets(Human)

GLP1R Tclin Glucagon-like peptide 1 receptor (1 Activities)

Discover Target: GLP1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin HERG (29587 Activities)

Discover Target: KCNH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GLP1R Tclin Glucagon-like peptide 1 receptor (111429 Activities)

Discover Target: GLP1R

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Associated Targets(non-human)

Mus musculus (284745 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Cynomolgus monkey (4946 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Names and Identifiers

IUPAC Name	2-[[4-[6-[(4-cyano-2-fluorophenyl)methoxy]pyridin-2-yl]piperidin-1-yl]methyl]-3-[[(2S)-oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid
INCHI	InChI=1S/C31H30FN5O4/c32-25-14-20(16-33)4-5-23(25)19-41-30-3-1-2-26(35-30)21-8-11-36(12-9-21)18-29-34-27-7-6-22(31(38)39)15-28(27)37(29)17-24-10-13-40-24/h1-7,14-15,21,24H,8-13,17-19H2,(H,38,39)/t24-/m0/s1
InChi Key	HYBAKUMPISVZQP-DEOSSOPVSA-N
Canonical SMILES	C1CN(CCC1C2=NC(=CC=C2)OCC3=C(C=C(C=C3)C#N)F)CC4=NC5=C(N4CC6CCO6)C=C(C=C5)C(=O)O
Isomeric SMILES	C1CO[C@@H]1CN2C3=C(C=CC(=C3)C(=O)O)N=C2CN4CCC(CC4)C5=NC(=CC=C5)OCC6=C(C=C(C=C6)C#N)F
Alternate CAS	2230198-02-2
PubChem CID	134611040
Molecular Weight	555.6

Certificates

Certificate of Analysis(COA)

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5 results found

Lot Number	Certificate Type	Date	Item
H2218501	Certificate of Analysis	Jun 05, 2022	P414495
H2218503	Certificate of Analysis	Jun 05, 2022	P414495
H2218504	Certificate of Analysis	Jun 05, 2022	P414495
H2218508	Certificate of Analysis	Jun 05, 2022	P414495
H2218546	Certificate of Analysis	Jun 05, 2022	P414495

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 100 mg/mL (179.98 mM); Ethanol: 100 mg/mL (179.98 mM); Water: Insoluble;

Safety and Hazards(GHS)

Pictogram(s)	GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P301+P312:IF SWALLOWED: call a POISON CENTER/doctor/... IF you feel unwell.

References

1. Zhang X, Belousoff MJ, Zhao P, Kooistra AJ, Truong TT, Ang SY, Underwood CR, Egebjerg T, Šenel P, Stewart GD et al.. (2020) Differential GLP-1R Binding and Activation by Peptide and Non-peptide Agonists.. Mol Cell, 80 (3): (485-500.e7). [PMID:33027691]
2. Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM et al.. (2022) A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.. J Med Chem, 65 (12): (8208-8226). [PMID:35647711]

Solution Calculators

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SKU	Size	Availability	Price
P414495-1mg	1mg	In stock	$240.90
P414495-5mg	5mg	In stock	$549.90
P414495-10mg	10mg	In stock	$858.90
P414495-25mg	25mg	In stock	$1,716.90
P414495-50mg	50mg	In stock	$2,746.90

PF-06882961 - 99%, high purity , CAS No.2230198-02-2, Agonist of GLP-1 receptor