β2AR agonist 7
β2AR agonist 7 is a MABA with both muscarinic acetylcholine M3 receptor antagonistic activity and β2-adrenergic receptor agonistic activity, with a Ki of 1.75 nM for hM3 and an EC50 of 0.054 nM for hβ2. β2AR agonist 7 binds to the M3 muscarinic receptor with high affinity and long-acting kinetic characteristics. β2AR agonist 7 induces smooth muscle relaxation and acts as a bronchoprotective agent against acute bronchoconstriction. β2AR agonist 7 can be used in the research of asthma and chronic obstructive pulmonary disease.
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- CAS. Nr.: 3109318-09-1
- Formel: C46H55N5O7S
- Molecular Weight:822.02
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
hM3 1.86 nM (Ki, 2 h incubation) |
hM3 1.75 nM (Ki, 24 h incubation) |
hM3 38 nM (Kb, 0.25 h preincubation) |
hM3 100 nM (Kb, 1 h preincubation) |
hβ2 0.054 nM (IC50, cAMP functional assay) |
In Vitro
β2AR agonist 7 (Compound 160) (2 h; 24 h) binds to human M3 receptors expressed on CHO cell membranes with high and sustained affinity, with a Ki value of 1.86 nM at 2 h and 1.75 nM at 24 h[1].
β2AR agonist 7 (0.25 h; 1 h) acts as a functional antagonist of human M3 receptors in CHO cells, with a KB value of 38.0 nM at 0.25 h and 100 nM at 1 h[1].
β2AR agonist 7 is a highly potent agonist of the human β2-adrenergic receptor, which induces intracellular cAMP accumulation with an EC50 of 0.054 nM[1].
The β2AR agonist 7 (0.5-10000 nM; tested via FLIPR calcium flux assay using CHO cells expressing hM3; single pre-incubation; 0.25 or 1 h) antagonizes acetylcholine (Acetylcholine chloride, HY-B0282)-induced hM3 signaling, with KB values of 38 nM and 100 nM, respectively[1].
β2AR agonist 7 (187 nM; isolated organ bath treatment; single treatment; monitored for 60 min with repeated carbachol stimulation) exhibits rapid onset and sustained vasodilatory effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Dunkin-Hartley guinea pigs, 6-7 weeks old, 350-400 g, acetylcholine-induced acute bronchoconstriction modified Einthoven model[1]
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Dosage:3 nmol/kg
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Administration:Intratracheal instillation, single administration, assessed at 1.5, 8 and 24 h
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Result:Attenuated acetylcholine-induced increases in Pao, Rrs and Ers and provided significant bronchoprotection at 1.5 h.
Bronchoprotection was largely maintained at 8 h, with residual protection remaining at 24 h.
Chemical Information
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CAS. Nr. 3109318-09-1
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Molecular Weight 822.02
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Formel C46H55N5O7S
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SMILES
C[C@@H](C1=CC=C(S(C2=CC=CC(OCCC(NC3=CC=C(CNC[C@H](O)C4=CC=C(O)C(N5)=C4C=CC5=O)C=C3)=O)=C2)(=O)=O)C=C1)N(CC6)CCN6C7CCCCCC7
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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)