Formoterol Hemifumarate

Catalog No.S2020

Formoterol Hemifumarate is a potent, selective and long-acting β2-adrenoceptor agonist to β2 and β1 receptors with pKd of 8.12 and 5.58, respectively.

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In DMSO USD 120 In stock
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Formoterol Hemifumarate Chemical Structure

Formoterol Hemifumarate Chemical Structure
Molecular Weight: 402.40

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Quality Control & MSDS

Related Compound Libraries

Formoterol Hemifumarate is available in the following compound libraries:

Product Information

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Product Description

Biological Activity

Formoterol hemifumarate is a potent, selective and long-acting β2-adrenoceptor agonist to β2 and β1 receptors with pKd of 8.12 and 5.58, respectively. Formoterol hemifumarate reveals 330-fold selectivity forβ2 over β1 receptors. Formoterol hemifumarate potently relaxes guinea pig trachea (pD2 = 9.29), and is longer-acting and 100-fold more potent than salbutamol. [1] Formoterol hemifumarate works like other β2-agonists, causing bronchodilation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. The long duration of formoterol action occurs because the formoterol molecules initially diffuse into the plasma membrane of the lung cells, and then are slowly released back outside, where they can come into contact with β2 adrenergic receptors. [2]

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-24)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02268396 Not yet recruiting COPD Pearl Therapeutics, Inc. November 2014 Phase 3
NCT02224157 Not yet recruiting Asthma AstraZeneca November 2014 Phase 3
NCT02196077 Recruiting Chronic Obstructive Pulmonary Disease (COPD) Pearl Therapeutics, Inc. August 2014 Phase 2
NCT02196714 Completed COPD Pearl Therapeutics, Inc. July 2014 Phase 1
NCT02149199 Suspended Asthma AstraZeneca July 2014 Phase 3

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Chemical Information

Download Formoterol Hemifumarate SDF
Molecular Weight (MW) 402.40
Formula

C19H24N2O4.1/2C4H4O4

CAS No. 43229-80-7
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 80 mg/mL (198 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(2-hydroxy-5-((S)-1-hydroxy-2-((S)-1-(4-methoxyphenyl)propan-2-ylamino)ethyl)phenyl)formamide hemifumaric acid

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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