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
USD 90 In stock
USD 370 In stock
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Formoterol Hemifumarate Chemical Structure

Formoterol Hemifumarate Chemical Structure
Molecular Weight: 402.40

Validation & Quality Control

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

SpeciesWeight (kg)Body Surface Area (m2)Km factor
Baboon120.620
Dog100.520
Monkey30.2412
Rabbit1.80.1512
Guinea pig0.40.058
Rat0.150.0256
Hamster0.080.025
Mouse0.020.0073
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

Value based on data from FDA Draft Guidelines: Center for Drug Evaluation and Research, Center for Biologics Evaluation and Research. (2002) Estimating the safe starting dose in clinical trials for therapeutics in adult healthy volunteers, U.S. Food and Drug Administration, Rockville, Maryland, USA.

For example, to convert the dose of resveratrol used in a mouse (22.4 mg/kg) to a dose based on surface area for 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)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02196077 Not yet recruiting Chronic Obstructive Pulmonary Disease (COPD) Pearl Therapeutics, Inc. August 2014 Phase 2
NCT02196714 Recruiting COPD Pearl Therapeutics, Inc. July 2014 Phase 1
NCT02149199 Recruiting Asthma AstraZeneca July 2014 Phase 3
NCT02062463 Recruiting Asthma Teva Pharmaceutical Industries|Teva Branded Pharmaceutical Products, R&D Inc. June 2014 Phase 4
NCT02157935 Recruiting COPD Patients AstraZeneca June 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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Tech Support & FAQs

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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