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Category:
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7TM Receptors Peptides (Gastrointestinal)Glucagon and Related Peptide ReceptorsGlucagon Receptor Compounds
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Cat.No.
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Product Name
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2311 |
L-168,049
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Price and Availability
Click here for full price details of
L-168049
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Chemical Name:
4-[3-(5-Bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-py
rrol-2-yl]pyridine |
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Biological Activity:
Very
potent and selective, non-competitive antagonist of the human glucagon receptor
(hGR). Binds with high affinity to human GR (IC50 = 3.7 nM), and
moderate affinity to murine and canine GRs (IC50 values are 63 and
60 nM respectively). In contrast, displays poor affinity for rat, guinea pig,
and rabbit glucagon receptors (IC50 > 1 μM). In functional studies, inhibits
glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC50
= 41 nM), and in murine liver membranes. Orally active in vivo.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Cascieri et al (1999) Characterization
of a novel, non-peptidyl antagonist of the human glucagon receptor.
J.Biol.Chem. 274 8694. de Laszlo et al (1999) Potent, orally absorbed glucagon receptor antagonists.
Bioorg.Med.Chem.Lett. 9 641. Dallas-Yang et al
(2001) Detection of glucagon-dependent GTPγS binding in high-throughput format. Anal.Biochem.
301 156.
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Keywords: L-168049, Peptides (Gastrointestinal), Potent, Orally Active Human Glucagon Receptor Antagonist, L168049, Tocris Bioscience
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