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GCGR-IN-17
CAS No. 1393124-08-7
GCGR-IN-17( PF-06291874 | PF06291874 | PF-6291874 )
Catalog No. M11636 CAS No. 1393124-08-7
A highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 59 | In Stock |
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| 5MG | 52 | In Stock |
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| 10MG | 76 | In Stock |
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| 100MG | Get Quote | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameGCGR-IN-17
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NoteResearch use only, not for human use.
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Brief DescriptionA highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR.
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DescriptionA highly potent glucagon receptor antagonist with Ki of 14 nM for hGCGR; shows excellent selectivity against a panel of 69 receptors, ion channels, uptake sites and enzymes; reduces the glucagon-elicited glucose excursion in a dose-dep endent manner in rats; displays low in vivo clearance and excellent oral bioavailability in both rats and dogs.Diabetes Phase 2 Discontinued.
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In Vitro——
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In VivoPF-06291874 exposure is approximately dose-proportional with a half-life of ～19.7-22.7 h. PF-06291874 has a fast on and off rate. PF-06291874 is highly bound to human plasma protein, with a mean free fraction of ～0.55%.
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SynonymsPF-06291874 | PF06291874 | PF-6291874
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PathwayGPCR/G Protein
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TargetGlucagon Receptor
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RecptorGlucagon Receptor
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Research AreaMetabolic Disease
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IndicationDiabetes
Chemical Information
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CAS Number1393124-08-7
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Formula Weight503.5134
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Molecular FormulaC26H28F3N3O4
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 30 mg/mL
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SMILESO=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C(C)=C2)N3C=C(C=N3)C(F)(F)F)CCC)C=C1)=O
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Chemical Nameglucagon receptor antagonists-4, N-[4-[(1S)-1-[3,5-dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy]butyl]benzoyl]-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Guzman-Perez A, et la. Bioorg Med Chem Lett. 2013 May 15;23(10):3051-8.
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