1443246-62-5 Usage
Description
VU0456810 is a compound with various applications across different industries, including pharmaceuticals and drug delivery systems. It is known for its unique properties that make it suitable for a range of uses.
Uses
Used in Pharmaceutical Industry:
VU0456810 is used as an anxiolytic drug for the treatment of epileptic seizures. It acts as a selective Kir3.1/3.2 (GIRK1/2) channel activator, demonstrating antiseizure activity and reducing anxiety-related behavior without sedative or addictive effects.
Used in Drug Delivery Systems:
VU0456810 is utilized in the development of novel drug delivery systems to enhance the efficacy and bioavailability of various pharmaceutical compounds. Its unique properties allow for improved delivery and therapeutic outcomes in targeted applications.
Used in Other Industries:
While the provided materials do not specify other industries where VU0456810 is used, its versatile nature suggests that it may have potential applications in areas such as cosmetics, agriculture, or materials science, where its specific properties can be harnessed for various purposes.
in vitro
in thallium flux assays, ml297 showed concentration-dependent efficacy when tested on cells expressing girk1/2. ml297 could also activate girk channels comprised of girk1/3 and girk1/4 subunit combinations. however, ml297 diaplayed a complete inability to modulate the activity of hek-293 cells expressing girk2 alone. a similar complete lack of efficacy was seen when ml297 was tested on hek-293 cells expressing girk2/3. therefore, it appeared that ml297 is only capable of activating girk channels containing a girk1 subunit [1].
in vivo
previous study performed an ascending dose study in mice and it was found that the animals appeared normal and not under obvious distress at all doses tested. ml297’s effects on locomotor activity as well as effects on motor function and coordination were further evaluated. results showed that ml297 at 60 mg/kg could immediate decrease in locomotor activity compared to the control group [1].
References
1) Wen?et al.?(2014),?Discovery of potent and selective GIRK1/2 modulators via “molecular switches’ within a series of 1-(3-cyclopropyl-1-phenyl-1H-pyrazol-5-yl)ureas; Bioorg. Med. Chem. Lett.,?24?5102
2) Kaufmann?et al. (2013),?ML-297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice; ACS Chem. Neurosci.,?4?1278
3) Wydeven?et al.?(2014),?Mechanisms underlying the activation of G-protein-gated inwardly rectifying K+ (GIRK) channels by the novel anxiolytic drug, ML297; Proc. Natl. Acad. Sci. USA,?111?10755
4) Psichas?et al.?(2016),?Galanin inhibits GLP-1 and GIP secretion via the GAL1 receptor in enteroendocrine L and K cells; Br. J. Pharmacol.,?173?888
Check Digit Verification of cas no
The CAS Registry Mumber 1443246-62-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,4,3,2,4 and 6 respectively; the second part has 2 digits, 6 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1443246-62:
(9*1)+(8*4)+(7*4)+(6*3)+(5*2)+(4*4)+(3*6)+(2*6)+(1*2)=145
145 % 10 = 5
So 1443246-62-5 is a valid CAS Registry Number.
