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
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Solvent & Solubility
- 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)
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (76.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (1.91 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (1.91 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.5285 mL | 7.6427 mL | 15.2854 mL | 38.2134 mL |
| 5 mM | 0.3057 mL | 1.5285 mL | 3.0571 mL | 7.6427 mL | |
| 10 mM | 0.1529 mL | 0.7643 mL | 1.5285 mL | 3.8213 mL | |
| 15 mM | 0.1019 mL | 0.5095 mL | 1.0190 mL | 2.5476 mL | |
| 20 mM | 0.0764 mL | 0.3821 mL | 0.7643 mL | 1.9107 mL | |
| 25 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5285 mL | |
| 30 mM | 0.0510 mL | 0.2548 mL | 0.5095 mL | 1.2738 mL | |
| 40 mM | 0.0382 mL | 0.1911 mL | 0.3821 mL | 0.9553 mL | |
| 50 mM | 0.0306 mL | 0.1529 mL | 0.3057 mL | 0.7643 mL | |
| 60 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6369 mL |
PF-610355 (hydrochloride) Related Classifications
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