4-[3-(5-BROMO-2-PROPOXYPHENYL)-5-(4-CHLOROPHENYL)-1H-PYRROL-2-YL]PYRIDINE
4-[3-(5-BROMO-2-PROPOXYPHENYL)-5-(4-CHLOROPHENYL)-1H-PYRROL-2-YL]PYRIDINE Basic information
- Product Name:
- 4-[3-(5-BROMO-2-PROPOXYPHENYL)-5-(4-CHLOROPHENYL)-1H-PYRROL-2-YL]PYRIDINE
- Synonyms:
-
- 4-[3-(5-BROMO-2-PROPOXYPHENYL)-5-(4-CHLOROPHENYL)-1H-PYRROL-2-YL]PYRIDINE
- L-168,049
- Pyridine, 4-[3-(5-bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]-
- 049
- L-168
- L-168049, 10 mM in DMSO
- Glucagon Receptor Antagonist II
- CAS:
- 191034-25-0
- MF:
- C24H20BrClN2O
- MW:
- 467.79
- Product Categories:
-
- Glucagon receptor and related
- Mol File:
- 191034-25-0.mol
4-[3-(5-BROMO-2-PROPOXYPHENYL)-5-(4-CHLOROPHENYL)-1H-PYRROL-2-YL]PYRIDINE Chemical Properties
- Boiling point:
- 542.3±50.0 °C(Predicted)
- Density
- 1.367±0.06 g/cm3(Predicted)
- storage temp.
- Store at RT
- solubility
- Soluble to 100 mM in DMSO and to 100 mM in ethanol
- form
- Light beige solid
- pka
- 13.99±0.50(Predicted)
- color
- Light yellow to yellow
4-[3-(5-BROMO-2-PROPOXYPHENYL)-5-(4-CHLOROPHENYL)-1H-PYRROL-2-YL]PYRIDINE Usage And Synthesis
Uses
L- is a potent (Kb = 25 nM), selective antagonist of glucagon.
Definition
ChEBI: 4-[3-(5-bromo-2-propoxyphenyl)-5-(4-chlorophenyl)-1H-pyrrol-2-yl]pyridine is a member of pyrroles.
Biological Activity
Very potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). Binds with high affinity to human GR (IC 50 = 3.7 nM), and moderate affinity to murine and canine GRs (IC 50 values are 63 and 60 nM respectively). In contrast, displays poor affinity for rat, guinea pig, and rabbit glucagon receptors (IC 50 > 1 μ M). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC 50 = 41 nM), and in murine liver membranes. Orally active in vivo .
in vivo
In the liver of L-G6pc /- mice, Pck1 mRNA expression is decreased by half 6 h after the administration of L-168049 (50 mg/kg body; p.o.), demonstrating the efficiency of the suppression of glucagon signaling. In agreement with the role of glucagon in the induction of extrahepatic gluconeogenesis, the administration of the L-168049 prevents the increase of the G6pc expression in both the kidneys and intestine of 6 h-fasted L-G6pc /- mice[3].
storage
Store at RT
4-[3-(5-BROMO-2-PROPOXYPHENYL)-5-(4-CHLOROPHENYL)-1H-PYRROL-2-YL]PYRIDINESupplier
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