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^[1][2][3].

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 Cl_int of 33 μL/min/mg^[2].

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

PF-610355 (0.1-1 μg; intratracheal; single dose) hydrochloride exhibits an intratracheal ED₅₀ of 0.1 μg for inhibiting acetylcholine-induced bronchoconstriction in anesthetized Beagle dogs, with a duration of action exceeding 8 hours at both ED₅₀ and 10× ED₅₀ doses and a therapeutic index of at least 10^[2].

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

654.22

C₃₄H₄₀ClN₃O₆S

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

Room temperature in continental US; may vary elsewhere.

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

• [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.