PF-610355 (hydrochloride)
PF-610355 hydrochloride is a β2-adrenergic receptor (β2-AR) full agonist with selectivity for β1-adrenergic receptors. PF-610355 hydrochloride increases intracellular cAMP levels, induces sustained tracheal smooth muscle relaxation, and inhibits acetylcholine-induced bronchoconstriction. PF-610355 hydrochloride can be used in research related to chronic obstructive pulmonary disease, asthma, and respiratory system diseases.
For research use only. We do not sell to patients.
- Formula: C34H40ClN3O6S
- Molecular Weight:654.22
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
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Beta-2 adrenergic receptor 0.26 nM (EC50) |
PF-610355 hydrochloride exhibits full agonist activity at human β2-adrenergic receptors in CHO cells with an EC50 of 0.26 nM, and has a β1/β2 selectivity ratio of 220[2].
The intrinsic clearance of PF-610355 hydrochloride in human liver microsomes is 54 μL/min/mg. Approximately 80% of phase I metabolism is mediated by CYP3A4, while glucuronidation also occurs, with a corresponding Clint of 33 μL/min/mg[2].
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:Beagle (female, 10-15 kg, anesthetized, artificially ventilated, acetylcholine-induced bronchoconstriction model)[2]
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Dosage:0.1 μg; 1 μg
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Administration:intratracheal; single dose
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Result:Achieved an ED50 of 0.1 μg for inhibiting acetylcholine-induced bronchoconstriction.
Demonstrated a duration of action of >8 hours at both 0.1 μg and 1 μg doses.
Showed no tachycardia at either tested dose.
Yielded a therapeutic index (lung vs. cardiovascular effects) of ≥10.
Chemical Information
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Appearance Solid
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Molecular Weight 654.22
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Formula C34H40ClN3O6S
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SMILES
O=C(NCC1=CC(C2=CC=C(O)C=C2)=CC=C1)CC3=CC=CC(CC(C)(NC[C@H](O)C4=CC=C(O)C(NS(=O)(C)=O)=C4)C)=C3.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
References
[1]. Fuso L, et al. Long-acting beta-agonists and their association with inhaled corticosteroids in COPD. Curr Med Chem. 2013;20(12):1477-1495. [Content Brief]
[2]. Glossop PA, et al. Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup. J Med Chem. 2010;53(18):6640-6652. [Content Brief]
[3]. Timalsina D, et al. Pharmacologic Activities of Plant-Derived Natural Products on Respiratory Diseases and Inflammations. Biomed Res Int. 2021;2021:1636816. Published 2021 Oct 4. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-610355 (hydrochloride) Related Classifications
HY-14296A Related Classifications
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