Indacaterol inhibits cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors with pEC50 of 8.06. Indacaterol inhibits electrically induced contraction on the electrically stimulated guinea pig trachea in a concentration-dependent manner with pEC50 of 8.23. Indacaterol induces a concentration-dependent inotropic effect with maximal efficacy of 75% in the isolated guinea pig left atrium . Indacaterol reverses the carbachol-induced contraction in a concentration-dependent manner with IC50 of 37 nM in human small airways. Indacaterol concentration dependently reverses the serotonin-induced contraction with IC50 of 10.5 nM in rat small airways. Indacaterol has the highest intrinsic efficacy of 53% in rat small airways and 73% in human small airways . Indacaterol (6.7 μg/kg) inhibits 5-HT-induced bronchoconstriction with a maximal effect of 85% in the conscious guinea pig. Indacaterol (12.5 μg/kg) dose-dependently inhibits methacholine-induced bronchoconstriction with a maximal effect of 85% in the anesthetized rhesus monkey
|Cell lines||HeLa (CCL-2), HEK293 (CRL-1573), and HT1080 (CCL-121) cells|
|Preparation method||The enzyme activities of MMP-9 in conditioned medium were determined by gelatin zymography protease assay. Briefly, cells (2 × 105 cells/well) were seeded in 6-well plates and allowed to grow to 80% confluency. The cells were then maintained in serum-free medium for 12 h prior to designated treatments with indacaterol and TNF-α for 24 h.|
|Incubation time||24 h|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||10 mM in DMSO|
Indacaterol inhibits tumor cell invasiveness and MMP-9 expression by suppressing IKK/NF-κB activation.
Lee SU, et al. Mol Cells. 2014 Aug;37(8):585-91. PMID: 25134539.
Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist, on small airways in human and rat precision-cut lung slices.
Sturton RG, et al. J Pharmacol Exp Ther. 2008 Jan;324(1):270-5. PMID: 17916760.
|Related Androgen Receptor Products|
Dehydroepiandrosterone is an effective antiapoptotic factor.
ASC-J9, also known as GO-Y025 and Dimethylcurcumin, suppressesing castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
GSK 2881078 is a selective androgen receptor modulator potentially for the treatment of cachexia. GSK 2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function.
Nandrolone phenylpropionate (NPP) is an anabolic-androgenic steroid. The low androgenicity and enhanced anabolic activity of NPP has shown to positively influence calcium metabolism and to increase bone mass in osteoporosis.
Testosterone is normally present in the circulation of both men and women. Due to the dynamic regulation of endogenous testosterone production, including the acute effects of competition and exercise, testosterone concentrations may vary considerably within and among individuals.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.