2. GPCR/G Protein
  3. GCGR
  4. L-168049

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.

For research use only. We do not sell to patients.

L-168049 Chemical Structure

L-168049 Chemical Structure

CAS No. : 191034-25-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
5 mg USD 140 In-stock
10 mg USD 230 In-stock
25 mg USD 480 In-stock
50 mg USD 820 In-stock
100 mg USD 1400 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

L-168049 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

IC50: 3.7 nM (human glucagon receptor), 63 nM (murine glucagon receptor), and 60 nM (canine glucagon receptor)[2]
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 Kb of 25 nM[2].

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

L-168049 Related Antibodies
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.
Molecular Weight

467.79

Formula

C24H20BrClN2O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1377 mL 10.6886 mL 21.3771 mL
5 mM 0.4275 mL 2.1377 mL 4.2754 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

L-168049 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-168049191034-25-0L168049L 168049GCGRGlucagon Receptornon-competitivenon-peptidylcAMPInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
L-168049
Cat. No.:
HY-103547
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.