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Arformoterol Tartrate

Name: Arformoterol Tartrate
Brand: Selleck Chemicals
SKU: S5217

Catalog No.S5217 Purity: 99.14%

Arformoterol Tartrate is the tartrate salt of arformoterol, a long-acting beta-2 adrenergic agonist with bronchodilator activity.

Arformoterol Tartrate Chemical Structure

CAS: 200815-49-2

Purity & Quality Control

Batch: Purity: 99.14%

99.14

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Biological Activity

Description	Arformoterol Tartrate is the tartrate salt of arformoterol, a long-acting beta-2 adrenergic agonist with bronchodilator activity.

In Vivo
In vivo	Arformoterol (R,R-formoterol) is a active isomer of racemic formoterol and is indicated for the long-term, maintenance treatment of bronchoconstriction in patients with COPD including chronic bronchitis and emphysema. It is a potent and selective agent which causes bronchial smooth muscle relaxation and inhibits the release of inflammatory mediators. Its pharmacological effects can be attributed to the increased intracellular cyclic adenosine monophosphate (cAMP) levels that result from the stimulation of intracellular adenyl cyclase. Arformoterol tartrate is well absorbed through lungs when administered by a nebulizer. The mean peak plasma concentration (Cmax) and systemic exposure (AUC0-12h) are 4.3 pg/mL and 34.5 pg.h/mL, respectively, when 15 µg arformoterol is administered every 12 h for 14 days in COPD patients. The time to achieve median steady state peak plasma concentration (tmax) is approximately half an hour after drug administration. The mean terminal half-life is 26 h in COPD patients when treated with 15 µg inhaled arformoterol twice daily for 14 days. The binding of arformoterol to human plasma proteins in vitro is 52-65% at concentrations of 0.25, 0.5 and 1.0 ng/mL of radiolabeled arformoterol. Metabolism occurs primarily by direct conjugation (glucuronidation) and secondary route of metabolism is via O-demethylation. Metabolism is mediated by atleast five human uridine diphosphoglucuronosyltransferase (UGT) isozymes as well as CYP2D6 and CYP2C19. After administration of a single oral dose of radiolabeled arformoterol, 63% of the radioactive amount was recovered in urine and 11% in feces within 48 h. A total of 89% of the total radioactive dose was recovered within 14 days, with 67% in urine and 22% in faeces^[1].
Animal Research	Animal Models	C57BL/6 male mice (8 wk old)
	Dosages	10 ng in 0.1 ml saline/20 g body weight
	Administration	instilled drop-wise in the external nares

References

[1] Rakesh Pahwa, et al. Tropical Journal of Pharmaceutical Research. 2010, 9(6):595-603.
[2] Weifeng Song, et al. Am J Respir Cell Mol Biol. 2011, 45(1): 88–94.

Chemical lnformation & Solubility

Molecular Weight	494.49	Formula	C₂₃H₃₀N₂O₁₀
CAS No.	200815-49-2	SDF	--
Smiles	CC(CC1=CC=C(C=C1)OC)NCC(C2=CC(=C(C=C2)O)NC=O)O.C(C(C(=O)O)O)(C(=O)O)O
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 99 mg/mL ( (200.2 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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