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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- CAS. Nr.: 1347232-69-2
- Formel: C39H43ClN4O9S2
- Molecular Weight:811.36
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
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β1 adrenoceptor 7.5 (pIC50) |
β2 adrenoceptor 9.1 (pIC50) |
β3 adrenoceptor 5.6 (pIC50) |
mAChR1 8.9 (pIC50) |
mAChR2 8.8 (pIC50) |
mAChR3 8.8 (pIC50) |
mAChR4 9.2 (pIC50) |
mAChR5 8.2 (pIC50) |
MMP9 |
IL-1β |
IL-8 |
In Vitro
LAS190792 exerts concentration-dependent anti-inflammatory effects in peripheral blood neutrophils derived from patients with chronic obstructive pulmonary disease and their matched controls, with -log IC50 values ranging from 6.8 to 10.3; moreover, when combined with non-effective concentrations of Fluticasone propionate (HY-B0154), it exerts synergistic anti-inflammatory effects in both of these two cell populations[1].
LAS190792 exhibits high-affinity non-selective binding to human M1-M4 muscarinic receptors (pIC50 range 8.8-9.2), has lower affinity for M5, and shows high-affinity selective binding to human β2-adrenergic receptors relative to the β1 and β3 subtypes (pIC50 = 9.1)[2].
LAS190792 shows potent antimuscarinic activity (pIC50 = 8.3) under β2-receptor blockade conditions, and it has a slower onset and longer duration of action than Batefenterol (HY-12980)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LAS190792 (0.03-10 µg/kg; administered via nebulization) exhibits potent bronchoprotective activity with an ED40 of 0.03 µg/kg, and has a wide safety margin, with transient blood glucose changes observed only at the highest tested dose[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagle (male, 12 kg)[2]
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Dosage:0.3 µg/kg; 1 µg/kg; 10 µg/kg; 30 µg/kg
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Administration:nebulized; single dose
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Result:Demonstrated dose-dependent bronchoprotection with an ID40 of 0.03 µg/kg at 30 min and a 13.3 h protective half-life, retaining obvious bronchoconstriction inhibition at 10 µg/kg for 24 h, with a safety margin of 333.
Caused minor irrelevant heart rate elevation below 10% at 10 µg/kg and marked heart rate rise over 10% only at 30 µg/kg.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1347232-69-2
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Molecular Weight 811.36
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Formel C39H43ClN4O9S2
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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
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Synonyms
AZD8999
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LAS190792 Related Classifications
HY-148527 Related Classifications
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