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Art. -Nr.: HY-184680

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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 K_i 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. Nr.: 3109318-04-6
Formel: C₄₅H₅₃N₅O₇S
Molecular Weight:808.00

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

β2AR agonist 6 Chemical Structure

CAS. Nr.: 3109318-04-6

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Biologische Aktivität
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- In Vitro
- In Vivo
Chemical Information
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Bioz

Biologische Aktivität

Beschreibung

In Vitro

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 K_i 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.

In Vivo

β2AR agonist 6 (compound 150) (3 nmol/kg; intratracheal instillation; single administration; measured at 1.5 h, 8 h and 24 h post-administration) attenuates acetylcholine (Acetylcholine chloride, HY-B0282)-induced increases in airway opening pressure, respiratory resistance and respiratory system elastance in male Dunkin-Hartley guinea pigs, and provides bronchoprotective effects lasting up to 24 h, which are comparable to those of Batefenterol (HY-12980)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Dunkin-Hartley guinea pigs, 6-7 weeks old, 350-400 g, acetylcholine-induced acute bronchoconstriction modified Einthoven model^[1]
Dosage:

3 nmol/kg
Administration:

Intratracheal instillation, single administration, assessed at 1.5, 8 and 24 h
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

CAS. Nr. 3109318-04-6
Molecular Weight 808.00
Formel C₄₅H₅₃N₅O₇S
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Frojuello Costa Bernstorff Damião MC, et al. Discovery and optimization of diarylsulfone-based dual M-Antagonists and β-Agonists (MABAs) as inhaled bronchodilators. European journal of medicinal chemistry. 2026 Jun 20;317:119082. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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