Carbenoxolone-d4

Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1, is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].

Product Specifications

UNSPSC

12352211

Target

11β-HSD; Amyloid-β; HIV

Type

Isotope-Labeled Compounds

Related Pathways

Anti-infection; Metabolic Enzyme/Protease; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Infection; Inflammation/Immunology; Neurological Disease

Solubility

10 mM in DMSO

Smiles

C[C@]12[C@@](C(C=C3[C@]2(CC[C@@]4([C@@]3([H])C[C@](C)(CC4)C(O)=O)C)C)=O)([H])[C@@]5([C@@](C(C)([C@H](CC5)OC(C([2H])([2H])C([2H])([2H])C(O)=O)=O)C)([H])CC1)C

Molecular Formula

C34H46D4O7

Molecular Weight

574.78

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Crespo Yanguas S, et al. TAT-Gap19 and Carbenoxolone Alleviate Liver Fibrosis in Mice. Int J Mol Sci. 2018 Mar 12;19 (3) . pii: E817.|[3]Hirata K, et al. Formulation of carbenoxolone for delivery to the skin. Int J Pharm. 2013 May 20;448 (2) :360-5.|[4]Kim J, et al. Protective effect of carbenoxolone on ER stress-induced cell death in hypothalamic neurons. Biochem Biophys Res Commun. 2015 Dec 25;468 (4) :793-9.|[5]Michalski K, et al. Carbenoxolone inhibits Pannexin1 channels through interactions in the first extracellular loop. J Gen Physiol. 2016 Feb;147 (2) :165-74.|[6]Pu J, et al. Antiviral activity of Carbenoxolone disodium against dengue virus infection. J Med Virol. 2017 Apr;89 (4) :571-581|[7]Sharma S, et al. Inhibition of Alzheimer's amyloid-beta aggregation in-vitro by carbenoxolone:Insight into mechanism of action. Neurochem Int. 2017 Sep;108:481-493.