AS1810722 is an orally active and potent STAT6 inhibitor with an IC 50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research
In Vitro
AS1810722 (compound 24) inhibits production of IL-4 with an IC 50 of 2.4 nM, but shows no effect on production of IFN-γ. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AS1810722 (compound 24; 0.03-0.3 mg/kg; orally; 30 min before, and 24h and 48 h after OVA exposure) suppress eosinophil infiltration in the lung in a dose-dependent manner in an antigen-induced mouse asthmatic model . AS1810722 inhibits in vitro Th2 differentiation with an IC 50 of 2.4 nM without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female Balb/c mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel Dosage: 0.03-0.3 mg/kg Administration: Orally; 30 min before, and 24 and 48 h after OVA exposure Result: Suppressed eosinophil infiltration in the lung in a dose-dependent manner.
Form:Solid
IC50& Target:STAT6 1.9 nM (IC 50 ) CYP3A4
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Klasse | Diazinanes |
| Subclass | Piperazines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Phenylpiperazines |
| Alternative Parents | Alpha amino acid amides N-arylpiperazines N-piperazineacetamides Pyrrolo[2,3-d]pyrimidines Aniline and substituted anilines Dialkylarylamines Aminopyrimidines and derivatives N-alkylpiperazines Fluorobenzenes Substituted pyrroles Aryl fluorides Heteroaromatic compounds Trialkylamines Primary carboxylic acid amides Azacyclic compounds Secondary amines Carbonyl compounds Organofluorides Organic oxides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Alpha-amino acid amide - Phenylpiperazine - N-arylpiperazine - Alpha-amino acid or derivatives - N-piperazineacetamide - Pyrrolo[2,3-d]pyrimidine - Pyrrolopyrimidine - Aniline or substituted anilines - Dialkylarylamine - Aminopyrimidine - Halobenzene - Fluorobenzene - N-alkylpiperazine - Pyrimidine - Substituted pyrrole - Aryl fluoride - Monocyclic benzene moiety - Aryl halide - Benzenoid - Heteroaromatic compound - Pyrrole - Amino acid or derivatives - Tertiary aliphatic amine - Carboxamide group - Tertiary amine - Primary carboxylic acid amide - Secondary amine - Carboxylic acid derivative - Azacycle - Organic nitrogen compound - Amine - Carbonyl group - Organic oxygen compound - Hydrocarbon derivative - Organic oxide - Organohalogen compound - Organofluoride - Organonitrogen compound - Organooxygen compound - Aromatic heteropolycyclic compound |
| Beschreibung | This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group. |
| External Descriptors | Not available |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Löslichkeit | DMSO : 62.5 mg/mL (130.89 mM; Need ultrasonic) |
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