β2AR agonist 6
β2AR agonist 6 is a MABA with both muscarinic acetylcholine M3 receptor antagonistic activity and β2 adrenergic receptor agonistic activity, with a Ki of 1.95 nM against hM3 and an EC50 of 0.266 nM against hβ2. β2AR agonist 6 binds to the M3 muscarinic receptor with high affinity and exhibits long-lasting binding, while displaying subnanomolar agonist activity at the β2 adrenergic receptor. β2AR agonist 6 induces smooth muscle relaxation and provides long-lasting bronchoprotective effects. β2AR agonist 6 can be used in research related to asthma and chronic obstructive pulmonary disease.
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- CAS No.: 3109318-04-6
- 화학식: C45H53N5O7S
- 분자량:808.00
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
β2AR agonist 6 (compound 150) (0.005-10000 nM; incubated with hM3-CHO cell membranes; single treatment; 2 or 24 h) exhibits sustained high-affinity binding to hM3[1].
β2AR agonist 6 (0.5-10000 nM; treatment of CHRM3-CHO cells; single pre-incubation; 0.25 or 1 h) antagonizes acetylcholine-induced calcium signals[1].
β2AR agonist 6 (0.005-10000 nM; tested in [3H]-NMS competitive binding assay using CHO cell membranes expressing hM3; single treatment; 2 or 24 h) binds to hM3, with Ki values of 1.89 nM and 1.95 nM after 2 h and 24 h of incubation, respectively[1].
β2AR agonist 6 (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-induced hM3 signaling, with KB values of 64.9 nM and 66.1 nM, respectively[1].
β2AR agonist 6 (0.5 pM-1 μM; β2 receptor cAMP/HTRF assay; single treatment; detection performed 1 h after 1 h of stimulation) activates hβ2 with an EC50 of 0.266 nM[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 generally maintained at 8 h, although Pao and Ers protection declined, and residual activity remained detectable at 24 h.
Chemical Information
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CAS No. 3109318-04-6
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분자량 808.00
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화학식 C45H53N5O7S
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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)CCN6C7CCCCC7
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
β2AR agonist 6 Related Classifications
HY-184680 Related Classifications
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