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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- No. CAS: 3109318-09-1
- Fòrmula: C46H55N5O7S
- Peso molecular:822.02
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Actividad biológica
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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) |
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.
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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No. CAS 3109318-09-1
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Peso molecular 822.02
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
β2AR agonist 7 Related Classifications
HY-184681 Related Classifications
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