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Purity: ≥98%
Danuglipron (PF-06882961; PF06882961) is a novel, non-peptide, allosteric and orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R). In an animal model that was humanized, it demonstrated similar effectiveness to injectable peptidic GLP-1R agonists. Type 2 diabetes (T2D) and obesity can be treated with an agonistic approach to the glucagon-like peptide-1 receptor (GLP-1R), which lowers blood sugar and causes weight loss.
| Targets |
GLP-1 receptor
|
|---|---|
| ln Vitro |
PF-06882961 promotes the accumulation of cAMP in CHO cells expressing the GLP-1Rs from both humans and monkeys with comparable EC50 values. On the other hand, PF-06882961 does not raise cAMP levels in GLP-1R-expressing mouse, rat, or rabbit cells.[2]
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| ln Vivo |
PF-06882961 decreases food intake and increases insulin release in response to glucose stimulation in monkeys.[2]
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| Cell Assay |
HEK293 cells that express hGLP-1R fused to green fluorescent protein (GFP) steadily (400,000 cells/well) are grown on 6-well plates for a full day and then stimulated for half a minute with PF-06882961. For these investigations, an agonist concentration of 1 μM that has been shown to cause maximal internalization is used. To test the endocytosis process' reversibility, cells are placed in specific wells, rinsed three times with PBS containing 0.1% BSA, and then incubated for a further two hours at 37 °C. After fixing the cells for 15 minutes at room temperature with 4% paraformaldehyde, the cells are cleaned three times using PBS containing 0.1% BSA.
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| Animal Protocol |
male cynomolgus monkeys
1 mg/kg, 5 mg/kg, 100 mg/kg IV, Oral gavage |
| References |
| Molecular Formula |
C31H30FN5O4
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|---|---|
| Molecular Weight |
555.599410533905
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| Exact Mass |
555.23
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| Elemental Analysis |
C, 67.01; H, 5.44; F, 3.42; N, 12.61; O, 11.52
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| CAS # |
2230198-02-2
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| Related CAS # |
2230198-02-2 (free acid); 2230198-03-3 (tris)
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| Appearance |
Solid powder
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| 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
|
| InChi Key |
HYBAKUMPISVZQP-DEOSSOPVSA-N
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| InChi Code |
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
|
| Chemical 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
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| Synonyms |
PF06882961; Danuglipron; PF 06882961; PF-06882961
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol: ~100 mg/mL
DMSO: ~10 mg/mL (~18 mM) |
|---|---|
| Solubility (In Vivo) |
5%DMSO + 40%PEG300 + 5%Tween 80: 5.0mg/ml (9.00mM) (Please use freshly prepared in vivo formulations for optimal results.)
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06153758 | Recruiting | Drug: Formulation A Drug: Formulation B |
Healthy Participants Healthy Subjects |
Pfizer | November 27, 2023 | Phase 1 |
Products are for research use only; We do not sell to patients
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