1393124-08-7

Basic information

• Product Name: glucagon receptor antagonists-4
• Synonyms: glucagon receptor antagonists-4;N-{4-[(1S)-1-{3,5-Dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy}butyl]benzoyl}-β-alanine;lucagon receptor antagonists-4;Glucagon Receptor Antagonist 4
• CAS NO: 1393124-08-7
• Molecular Formula: C₂₆H₂₈F₃N₃O₄
• Molecular Weight: 503.5134296
• Product Categories: API
• Mol File: 1393124-08-7.mol
• Article Data: 1

Chemical Properties

• Boiling Point: 675.0±55.0 °C(Predicted)
• Appearance: /
• Density: 1.27±0.1 g/cm3(Predicted)
• PKA: 4.28±0.10(Predicted)
• CAS DataBase Reference: glucagon receptor antagonists-4(CAS DataBase Reference)
• NIST Chemistry Reference: glucagon receptor antagonists-4(1393124-08-7)
• EPA Substance Registry System: glucagon receptor antagonists-4(1393124-08-7)

Safety Data

• Hazardous Substances Data: 1393124-08-7(Hazardous Substances Data)

Usage

Description

Glucagon receptor antagonists-4, specifically PF-06291874, is a novel and potent compound designed to target and block the glucagon receptor. This antagonist has been developed for the potential treatment of diabetes mellitus. It is characterized by its lower molecular weight and lipophilicity compared to previous glucagon receptor antagonists, which contributes to its excellent selectivity in broad-panel screening. Additionally, PF-06291874 demonstrates lower cytotoxicity and has shown excellent overall in vivo safety in early pre-clinical testing.

Uses

Used in Pharmaceutical Industry:
Glucagon receptor antagonists-4, such as PF-06291874, are used as therapeutic agents for the treatment of diabetes mellitus. The compound works by blocking the glucagon receptor, which helps regulate blood glucose levels. This antagonist's lower molecular weight and lipophilicity result in improved selectivity and reduced cytotoxicity, making it a promising candidate for further development and potential clinical use in managing diabetes.
Used in Research and Development:
In the field of research and development, glucagon receptor antagonists-4 like PF-06291874 are utilized for studying the role of glucagon receptors in various physiological processes and their potential as targets for therapeutic intervention. The compound's excellent selectivity and safety profile make it a valuable tool for investigating the underlying mechanisms of diabetes and other related conditions.
Used in Drug Delivery Systems:
Similar to gallotannin, glucagon receptor antagonists-4 may also benefit from novel drug delivery systems to enhance their applications and efficacy. These systems could involve the use of organic or metallic nanoparticles as carriers for the delivery of PF-06291874, aiming to improve its delivery, bioavailability, and therapeutic outcomes in the treatment of diabetes mellitus.

Upstream product

• 1383800-57-4 ethyl 4-butyrylbenzoate 
• 51934-41-9 4-iodobenzoic acid ethyl ester 
• 1355533-73-1 ethyl 4-(1-hydroxybutyl)benzoate 
• 1393131-62-8 C₂₈H₃₂F₃N₃O₄ 
• 1393125-31-9 1-(4-bromo-2,6-dimethylphenyl)-4-(trifluoromethyl)-1H-pyrazole 
• 24596-19-8 4-bromo-2,6-dimethylphenylamine 
• 1393125-42-2 3,5-dimethyl-4-(4-(trifluoromethyl)-1H-pyrazol-1-yl)phenol 
• 1393126-81-2 C₁₆H₂₃NO₄ 
• 1393126-80-1 (R)-4-(1-hydroxybutyl)benzoic acid 
• 1393125-60-4 C₁₃H₁₈O₃ 

Relevant articles and documents

The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus

A novel and potent small molecule glucagon receptor antagonist for the treatment of diabetes mellitus is reported. This candidate, (S)-3-[4-(1-{3,5- dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy}butyl)benzamido] propanoic acid, has lower molecular weight and lipophilicity than historical glucagon receptor antagonists, resulting in excellent selectivity in broad-panel screening, lower cytotoxicity, and excellent overall in vivo safety in early pre-clinical testing. Additionally, it displays low in vivo clearance and excellent oral bioavailability in both rats and dogs. In a rat glucagon challenge model, it was shown to reduce the glucagon-elicited glucose excursion in a dose-dependent manner and at a concentration consistent with its rat in vitro potency. Its properties make it an excellent candidate for further investigation.