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L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $39 | In Stock | In Stock | |
| 5 mg | $89 | In Stock | In Stock | |
| 10 mg | $147 | In Stock | In Stock | |
| 25 mg | $313 | In Stock | In Stock | |
| 50 mg | $562 | In Stock | In Stock | |
| 100 mg | $843 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $125 | In Stock | In Stock |
| Description | L-168049 is a selective and non-competitive antagonist of human glucagon receptor with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine, respectively. |
| Targets&IC50 | Glucagon receptor (murine):63 nM (IC50), Glucagon receptor (human):3.7 nM (IC50), Glucagon receptor (canine):60 nM (IC50) |
| In vitro | In Chinese hamster ovary cells expressing the human glucagon receptor, L-168049 increases the apparent EC50 of glucagon-stimulated adenylate cyclase and decreases maximal glucagon stimulation with a Kb of 25 nM[1]. L-168049 blocks glucagon-stimulated cAMP formation in mouse liver membrane and inhibits glucagon (100 pM)-stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor with IC50 of 41 nM [3]. |
| In vivo | In the liver of L-G6pc-/- mice, L-168049 (50 mg/kg body; p.o.) reduces Pck1 mRNA expression by half within 6 hours. L-168049 prevents the increase in G6pc expression in the kidney and gut [2]. |
| Synonyms | L-168,049 |
| Molecular Weight | 467.79 |
| Formula | C24H20BrClN2O |
| Cas No. | 191034-25-0 |
| Smiles | CCCOc1ccc(Br)cc1-c1cc([nH]c1-c1ccncc1)-c1ccc(Cl)cc1 |
| Relative Density. | 1.367g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||
| Solubility Information | Ethanol: 3.4 mM, Sonication is recommended. DMSO: insoluble | ||||||||||
Solution Preparation Table | |||||||||||
Ethanol
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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