Art. -Nr.: HY-103547

L-168049

1 Cited Publications

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

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Reinheit: 99.94%
CAS. Nr.: 191034-25-0
Formel: C₂₄H₂₀BrClN₂O
Molecular Weight:467.79

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

L-168049 Chemical Structure

CAS. Nr.: 191034-25-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 3.7 nM (human glucagon receptor), 63 nM (murine glucagon receptor), and 60 nM (canine glucagon receptor)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.007 μM Compound: 49	Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2 Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2	[PMID: 10201821]
CHO	IC₅₀	0.037 μM Compound: 49	Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2 Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2	[PMID: 10201821]
CHO	IC₅₀	0.17 μM Compound: 49	Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2 Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2	[PMID: 10201821]
CHO	IC₅₀	0.25 μM Compound: 49	Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2	[PMID: 10201821]

In Vitro

L-168049 (compound 49) inhibits glucagon (100 pM) stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor (hGIAR) (IC₅₀ of 41 nM). L-168049 blocks cAMP formation stimulated by glucagon in murine liver membranes^[1].
L-168049 increases the apparent EC₅₀ for glucagon stimulation of adenylyl cyclase in Chinese hamster ovary cells expressing the human glucagon receptor and decreases the maximal glucagon stimulation observed, with a K_b of 25 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 191034-25-0
Appearance Solid
Molecular Weight 467.79
Formel C₂₄H₂₀BrClN₂O
Color Light yellow to yellow
SMILES

ClC1=CC=C(C2=CC(C3=CC(Br)=CC=C3OCCC)=C(C4=CC=NC=C4)N2)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (106.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1377 mL

10.6886 mL

21.3771 mL

5 mM

0.4275 mL

2.1377 mL

4.2754 mL

10 mM

0.2138 mL

1.0689 mL

2.1377 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. S E de Laszlo, et al. Potent, orally absorbed glucagon receptor antagonists. Bioorg Med Chem Lett. 1999 Mar 8;9(5):641-6. [Content Brief]

[2]. M A Cascieri, et al. Characterization of a novel, non-peptidyl antagonist of the human glucagon receptor. J Biol Chem. 1999 Mar 26;274(13):8694-7. [Content Brief]

[3]. Elodie Mutel, et al. Control of blood glucose in the absence of hepatic glucose production during prolonged fasting in mice: induction of renal and intestinal gluconeogenesis by glucagon. Diabetes. 2011 Dec;60(12):3121-31. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1377 mL	10.6886 mL	21.3771 mL	53.4428 mL
	5 mM	0.4275 mL	2.1377 mL	4.2754 mL	10.6886 mL
	10 mM	0.2138 mL	1.0689 mL	2.1377 mL	5.3443 mL
	15 mM	0.1425 mL	0.7126 mL	1.4251 mL	3.5629 mL
	20 mM	0.1069 mL	0.5344 mL	1.0689 mL	2.6721 mL
	25 mM	0.0855 mL	0.4275 mL	0.8551 mL	2.1377 mL
	30 mM	0.0713 mL	0.3563 mL	0.7126 mL	1.7814 mL
	40 mM	0.0534 mL	0.2672 mL	0.5344 mL	1.3361 mL
	50 mM	0.0428 mL	0.2138 mL	0.4275 mL	1.0689 mL
	60 mM	0.0356 mL	0.1781 mL	0.3563 mL	0.8907 mL
	80 mM	0.0267 mL	0.1336 mL	0.2672 mL	0.6680 mL
	100 mM	0.0214 mL	0.1069 mL	0.2138 mL	0.5344 mL

Keywords

L-168049

1 Cited Publications

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L-168049

Orally Active Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Publications Citing Use of MedChemExpress (MCE) L-168049

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

L-168049

Orally Active Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

GPCR/G Protein Compound Library

Publications Citing Use of MedChemExpress (MCE) L-168049

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

L-168049 Related Classifications

HY-103547 Related Classifications