5438-71-1

Usage

InChI:InChI=1/C11H14N4O4/c1-14-9-8(10(18)15(2)11(14)19)12-6(13-9)4-3-5-7(16)17/h3-5H2,1-2H3,(H,12,13)(H,16,17)

Upstream product

• 5440-00-6 4,5-Diamino-1,3-dimethyluracil 
• 53715-97-2 5,5'-oxybis(5-oxopentanoic acid) 
• 108-55-4 glutaric anhydride, 
• 109418-98-6 5-(6-amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-ylamino)-5-oxopentanoic acid 

Relevant academic research and scientific papers

Scaffold Hopping and Optimization of Maleimide Based Porcupine Inhibitors

Porcupine is an O-acyltransferase that regulates Wnt secretion. Inhibiting porcupine may block the Wnt pathway which is often dysregulated in various cancers. Consequently porcupine inhibitors are thought to be promising oncology therapeutics. A high throughput screen against porcupine revealed several potent hits that were confirmed to be Wnt pathway inhibitors in secondary assays. We developed a pharmacophore model and used the putative bioactive conformation of a xanthine inhibitor for scaffold hopping. The resulting maleimide scaffold was optimized to subnanomolar potency while retaining good physical druglike properties. A preclinical development candidate was selected for which extensive in vitro and in vivo profiling is reported.

SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF

Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.

Fluorescence immunoassays using fluorescent dyes free of aggregation and serum binding

Fluorescence immunoassays methods are provided which use fluorescent dyes which are free of aggregation and serum binding. Such immunoassay methods are thus, particularly useful for the assay of biological fluids, such as serum, plasma, whole blood and urine.

Aminoalkylmaleimides and hapten and antigen derivatives derived therefrom as well as conjugates with peptides or proteins

The invention concerns new aminoalkylmaleimides of the general formula I STR1 in which R1 and R2 are the same or different and represent hydrogen or a C1 -C4 alkyl group and A represents a straight-chain or branched, saturated or unsaturated alkylene group with 2 to 6 carbon atoms which is interrupted, if desired, by an oxygen or sulphur atom or a carbonyl group, as well as their corresponding acid addition salts. The present invention also concerns amidoalkylmaleimide derivatives formed from compounds of the general formula I and immunological binding partners. In addition, the invention concerns immunological conjugates which can be produced by reaction of the amidoalkylmaleimide derivatives with peptides or proteins. The subject matter of the present invention are also the corresponding processes of production of the compounds according to the present invention as well as the use of these conjugates in diagnostic methods of determination, in particular in immunoassays.

Structure-Activity Relationships of 1,3-Dialkylxanthine Derivatives at Rat A3 Adenosine Receptors

1,3-Dialkylxanthine analogues containing carboxylic acid and other charged groups on 8-position substituents were synthesized.These derivatives were examined for affinity in radioligand binding assays at rat brain A3 adenosine receptors stably

Divalent hapten derivatives

Divalent hapten derivatives wherein two hapten moieties are connected by means of a bifunctional spacer wherein the derivative has the formula where A is a bonded hapten moiety and X is a bifunctional spacer having the formula where m is independently 0 o