PF-610355 (hydrochloride)
Based on 1 Customer Validation
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
Description
IC50 & Target
[2]|
Beta-2 adrenergic receptor 0.26 nM (EC50) |
In Vitro
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. .
In Vivo
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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