1347232-69-2
Chemical Structure
LAS190792
Synonym(s): AZD8999
- CAS No.: 1347232-69-2
- Formula:C39H43ClN4O9S2
- Molecular Weight:811.36
IUPAC Name: 3-ethylpyridazine-4-carboxylic acid
InChIKey: SNXJYSXRLKUBSZ-WBXFWKJNSA-N
SMILES: COC(C=C(NC(OCCN(C)[C@@H]1CC[C@@H](OC(C(O)(C2=CC=CS2)C3=CC=CS3)=O)CC1)=O)C(Cl)=C4)=C4CNC[C@H](O)C5=CC=C(O)C(N6)=C5C=CC6=O
Biological Activity: LAS190792 is a bifunctional muscarinic acetylcholine receptor (mAChR) antagonist and β2-adrenergic receptor agonist. LAS190792 has a pIC50 of 8.8 against human M3 muscarinic receptor and a pIC50 of 9.1 against human β2-adrenergic receptor. LAS190792 exhibits vasodilatory and anti-inflammatory activities, and induces sustained bronchodilation in dogs. LAS190792 inhibits the release of IL-8, MMP9, IL-1β and GM-CSF from lipopolysaccharide-stimulated neutrophils. LAS190792 can be used in research related to respiratory system diseases[1][2][3].
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LAS190792 | LAS190792 is a bifunctional muscarinic acetylcholine receptor (mAChR) antagonist and β2-adrenergic receptor agonist. LAS190792 has a pIC50 of 8.8 against human M3 muscarinic receptor and a pIC50 of 9.1 against human β2-adrenergic receptor. LAS190792 exhibits vasodilatory and anti-inflammatory activities, and induces sustained bronchodilation in dogs. LAS190792 inhibits the release of IL-8, MMP9, IL-1β and GM-CSF from lipopolysaccharide-stimulated neutrophils. LAS190792 can be used in research related to respiratory system diseases. | |||||||||||||||||||||
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- [1]. Milara J, et al. In vitro anti-inflammatory effects of AZD8999, a novel bifunctional muscarinic acetylcholine receptor antagonist /β2-adrenoceptor agonist (MABA) compound in neutrophils from COPD patients. PloS one. 2019;14(1):e0210188. [Content Brief]
- [2]. Aparici M, et al. Pharmacological preclinical characterization of LAS190792, a novel inhaled bifunctional muscarinic receptor antagonist /β2-adrenoceptor agonist (MABA) molecule. Pulmonary Pharmacology & Therapeutics, 2017, 46: 1-10.
- [3]. Gavaldà A, et al. Bronchoprotective activity and safety assessment of two novel dual-acting MABA compounds (LAS190792 and LAS191351) in dogs. European Respiratory Journal, 2014, 44(Suppl 58): 4864.
Keywords
