β2-adrenoceptor agonist 1
β2-adrenoceptor agonist 1 is a β2-adrenoceptor agonist with an EC50 of 7 pM. β2-adrenoceptor agonist 1 induces cAMP accumulation and airway/tracheal smooth muscle relaxation. β2-adrenoceptor agonist 1 inhibits inflammatory cell activity, reduces inflammatory cytokine production, and decreases mast cell infiltration. β2-adrenoceptor agonist 1 can be used for asthma research.
For research use only. We do not sell to patients.
- Formula: C22H28N2O5
- Molecular Weight:400.47
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Storage:
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
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All Adrenergic Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
β2 adrenoceptor 7 pM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BEAS-2B | CC50 |
50.07 μM
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Cytotoxicity against human bronchial epithelial BEAS-2B cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay.
Cytotoxicity against human bronchial epithelial BEAS-2B cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay.
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j.ejmech.2026.119297 |
| HEK-293T | CC50 |
33.39 μM
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Cytotoxicity against human embryonic kidney HEK293T cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay.
Cytotoxicity against human embryonic kidney HEK293T cells assessed as viability reduction after 48 hrs incubation by CCK-8 assay.
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j.ejmech.2026.119297 |
In Vitro
β2-adrenoceptor agonist 1 (Compound C3) (7 pM; 60 min) acts as a potent β2-AR agonist in HEK293 cells overexpressing human β2-AR, with an EC50 of 7 pM and high β2/β1 selectivity[1].
β2-adrenoceptor agonist 1 relaxes Histamine (HY-B1204)-precontracted isolated guinea pig tracheal strips with Emax = 136.88% and pD2 = 8.32[1].
β2-adrenoceptor agonist 1 (10-20 μM; 48 h) has low cytotoxicity in BEAS-2B and HEK293T cells, with CC50 values of 50.07 μM and 33.39 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Human bronchial epithelial BEAS-2B and human embryonic kidney HEK293T cells
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Concentration:10 μM; 20 μM
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Incubation Time:48 h (C3); 2 h (CCK-8)
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Result:At 10 μM, C3 was non-cytotoxic in BEAS-2B and showed no significant cytotoxicity in HEK293T cells.
At 20 μM, C3 remained non-toxic in BEAS-2B, whereas HEK293T cells showed dose-dependent cytotoxicity.
C3 CC50 = 50.07 μM in BEAS-2B and 33.39 μM in HEK293T.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old)[1]
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Dosage:100 μg/kg/day (228.9 nmol/kg/day); 200 μg/kg/day (458.5 nmol/kg/day)
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Administration:inhalation; once daily; 15 days
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Result:At 100 μg/kg/day, compound C3 did not improve lung function in asthmatic mice.
At 200 μg/kg/day, compound C3 improved Peak Expiratory Flow (PEF), Maximal Mid-Expiratory Flow (MMEF), Dynamic Compliance (Cdyn), Forced Vital Capacity (FVC), and Forced Expiratory Volume in 0.1 s (FEV0.1) to levels comparable to the positive-control group.
Both 100 and 200 μg/kg/day compound C3 reduced total white blood cell count in bronchoalveolar lavage fluid (BALF).
Differential cell counting showed reductions in eosinophils, neutrophils, and lymphocytes in groups receiving compound C3 compared with the model group.
Compound C3 reduced IL-4, IL-5, and IL-13 levels in BALF, lung tissue, and serum, with the 200 μg/kg/day group showing efficacy comparable to the positive control.
Toluidine blue (HY-D0220) staining showed dose-dependent improvement in lung histopathology, and the 200 μg/kg/day group had a reduction in mast cell numbers comparable to the positive control.
H&E staining confirmed protective effects on lung histopathology; the 200 μg/kg/day group showed an effect comparable to the positive control.
Chemical Information
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Molecular Weight 400.47
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Formula C22H28N2O5
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SMILES
COC1=C(C=CC=C1)CCC(NCC(C2=CC=C(C3=C2OCC(N3)=O)O)O)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
β2-adrenoceptor agonist 1 Related Classifications
HY-189674 Related Classifications
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