Home >> Research Area >>GPCR/G protein>>Glucagon Receptor>> glucagon receptor antagonists 2

glucagon receptor antagonists 2

Glucagon receptor antagonist,highly potent CAS# 202917-18-8

glucagon receptor antagonists 2

Catalog No. BCC1594----Order now to get a substantial discount!

Product Name & Size Price Stock
glucagon receptor antagonists 2: 5mg $253 In Stock
glucagon receptor antagonists 2: 10mg Please Inquire In Stock
glucagon receptor antagonists 2: 20mg Please Inquire Please Inquire
glucagon receptor antagonists 2: 50mg Please Inquire Please Inquire
glucagon receptor antagonists 2: 100mg Please Inquire Please Inquire
glucagon receptor antagonists 2: 200mg Please Inquire Please Inquire
glucagon receptor antagonists 2: 500mg Please Inquire Please Inquire
glucagon receptor antagonists 2: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of glucagon receptor antagonists 2

Number of papers citing our products

Chemical structure

glucagon receptor antagonists 2

3D structure

Chemical Properties of glucagon receptor antagonists 2

Cas No. 202917-18-8 SDF Download SDF
PubChem ID 66577053 Appearance Powder
Formula C22H30FNO2 M.Wt 359.49
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 16.67 mg/mL (46.37 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
Chemical Name 5-fluoro-2-[(4S)-3-[(1R)-1-hydroxyethyl]-2,6-di(propan-2-yl)-5-propyl-1,4-dihydropyridin-4-yl]phenol
SMILES CCCC1=C(NC(=C(C1C2=C(C=C(C=C2)F)O)C(C)O)C(C)C)C(C)C
Standard InChIKey OINVVPOIGFSNHM-VLIAUNLRSA-N
Standard InChI InChI=1S/C22H32FNO2/c1-7-8-17-20(16-10-9-15(23)11-18(16)26)19(14(6)25)22(13(4)5)24-21(17)12(2)3/h9-14,20,24-26H,7-8H2,1-6H3/t14-,20+/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of glucagon receptor antagonists 2

DescriptionGlucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist.

References:
[1]. Ladouceur, Gaetan H. et al. Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists. Bioorganic & Medicinal Chemistry Letters (2002), 12(23), 3421-3424.

glucagon receptor antagonists 2 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

glucagon receptor antagonists 2 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of glucagon receptor antagonists 2

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7817 mL 13.9086 mL 27.8172 mL 55.6344 mL 69.543 mL
5 mM 0.5563 mL 2.7817 mL 5.5634 mL 11.1269 mL 13.9086 mL
10 mM 0.2782 mL 1.3909 mL 2.7817 mL 5.5634 mL 6.9543 mL
50 mM 0.0556 mL 0.2782 mL 0.5563 mL 1.1127 mL 1.3909 mL
100 mM 0.0278 mL 0.1391 mL 0.2782 mL 0.5563 mL 0.6954 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on glucagon receptor antagonists 2

highly potent glucagon receptor antagonist

Featured Products
New Products
 

References on glucagon receptor antagonists 2

Discovery of a Novel Series of Orally Bioavailable and CNS Penetrant Glucagon-like Peptide-1 Receptor (GLP-1R) Noncompetitive Antagonists Based on a 1,3-Disubstituted-7-aryl-5,5-bis(trifluoromethyl)-5,8-dihydropyrimido[4,5-d]pyrim idine-2,4(1H,3H)-dione Core.[Pubmed:28103022]

J Med Chem. 2017 Feb 23;60(4):1611-1616.

A duplexed, functional multiaddition high throughput screen and subsequent optimization effort identified the first orally bioavailable and CNS penetrant glucagon-like peptide-1 receptor (GLP-1R) noncompetitive antagonist. Antagonist 5d not only blocked exendin-4-stimulated insulin release in islets but also lowered insulin levels while increasing blood glucose in vivo.

Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists.[Pubmed:25127101]

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4266-70.

Furan-2-carbohydrazides were found as orally active glucagon receptor antagonists. Starting from the hit compound 5, we successfully determined the structure activity relationships of a series of derivatives obtained by modifying the acidity of the phenol. We identified the ortho-nitrophenol as a good scaffold for glucagon receptor inhibitory activity. Our efforts have led to the discovery of compound 7l as a potent glucagon receptor antagonist with good bioavailability and satisfactory long half-life.

Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.[Pubmed:22030028]

Bioorg Med Chem Lett. 2011 Dec 1;21(23):7124-30.

A novel class of N-aryl-2-acylindole human glucagon receptor (hGCGR) antagonists is reported. These compounds demonstrate good pharmacokinetic profiles in multiple preclinical species. One compound from this series, indole 33, is orally active in a transgenic murine pharmacodynamic model. Furthermore, a 1mg/kg oral dose of indole 33 lowers ambient glucose levels in an ob/ob/hGCGR transgenic murine diabetes model. This compound was deemed suitable for preclinical safety studies and was found to be well tolerated in an 8-day experimental rodent tolerability study. The combination of preclinical efficacy and safety observed with compound 33 highlights the potential of this class as a treatment for type 2 diabetes.

Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide.[Pubmed:12477359]

J Med Chem. 2002 Dec 19;45(26):5755-75.

Highly potent human glucagon receptor (hGluR) antagonists have been prepared employing both medicinal chemistry and targeted libraries based on modification of the core (proximal) dimethoxyphenyl group, the benzyl ether linkage, as well as the (distal) benzylic aryl group of the lead 2, 3-cyano-4-hydroxybenzoic acid (3,5-dimethoxy-4-isopropylbenzyloxybenzylidene)hydrazide. Electron-rich proximal aryl moieties such as mono- and dimethoxy benzenes, naphthalenes, and indoles were found to be active. The SAR was found to be quite insensitive regarding the linkage to the distal aryl group, since long and short as well as polar and apolar linkers gave highly potent compounds. The presence of a distal aryl group was not crucial for obtaining high binding affinity to the hGluR. In many cases, however, the affinity could be further optimized with substituted distal aryl groups. Representative compounds have been tested for in vitro metabolism, and structure-metabolism relationships are described. These efforts lead to the discovery of 74, NNC 25-2504, 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide, with low in vitro metabolic turnover. 74 was a highly potent noncompetitive antagonist of the human glucagon receptor (IC(50) = 2.3 nM, K(B) = 760 pM) and of the isolated rat receptor (IC(50) = 430 pM, K(B) = 380 pM). Glucagon-stimulated glucose production from isolated primary rat hepatocytes was inhibited competitively by 74 (K(i) = 14 nM). This compound was orally available in dogs (F(po) = 15%) and was active in a glucagon-challenged rat model of hyperglucagonemia and hyperglycemia.

Description

Glucagon receptor antagonists-2 is a highly potent glucagon receptor antagonist.

Keywords:

glucagon receptor antagonists 2,202917-18-8,Natural Products,Glucagon Receptor, buy glucagon receptor antagonists 2 , glucagon receptor antagonists 2 supplier , purchase glucagon receptor antagonists 2 , glucagon receptor antagonists 2 cost , glucagon receptor antagonists 2 manufacturer , order glucagon receptor antagonists 2 , high purity glucagon receptor antagonists 2

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: