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Fiduxosin

Catalog No. T11286   CAS 208993-54-8
Synonyms: A 185980.1, ABT 980

Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.

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Fiduxosin Chemical Structure
Fiduxosin, CAS 208993-54-8
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1 mg In stock $ 700.00
5 mg In stock $ 1,800.00
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Purity: 99.73%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Fiduxosin is a selective and potent α1-adrenoceptor antagonist with inhibitory effects on α1a-adrenoceptor, α1b-adrenoceptor and α1d-adrenoceptor, with Ki values of 0.160 nM, 24.9 nM and 0.920 nM, respectively. Fiduxosin can be used for the treatment of benign prostatic hyperplasia.
Targets&IC50 α2b-adrenoceptor:21 nM (Ki,Rat), 5HT1A receptor:29 nM (Ki,Rat), α2a-adrenoceptor:92 nM (Ki,Human), α1b- adrenoceptor:24.9 nM (Ki), α2c-adrenoceptor:22 nM (Ki,Human), α1d-adrenoceptor:0.92 nM (Ki), α1a-adrenoceptor:0.16 nM (Ki)
In vitro Fiduxosin, in addition to β-adrenoceptors (2-5 μM), exhibits low affinity for other adrenoceptors, including cloned human α2a-adrenoceptors (92 nM), α2c-adrenoceptors (22 nM), and rat neonatal lung α2b-adrenoceptors (21 nM). Moreover, Fiduxosin shows low affinity for 5HT1A receptors in rat cortex (29 nM) compared to its affinity at α1a-adrenoceptors (0.16 nM). In the rabbit urethra, Fiduxosin competitively antagonizes PE-induced responses with a pA2 value of 7.58[2].
In vivo In anesthetized dogs, Fiduxosin (i.v.) at doses of 30, 100, and 300 μg/kg antagonizes intraurethral pressure (IUP) responses to intravenous epinephrine (EPI). Transient effects on blood pressure are observed with Fiduxosin at doses of 178, 592, and 1780 μg/kg (i.v.) in spontaneously hypertensive rats (SHR), with the lowest dose having no effect on mean arterial pressure (MAP).In SHR, Fiduxosin at a dose of 3 μmol/kg or 1780 μg/kg (i.v.) causes a slight reduction in MAP. However, head-up tilt results in a further diminution of MAP at the 15-minute observation point, with minimal additional changes observed at times ≥30 minutes postdosing.When administered orally at doses of 0.1, 0.3, 1.0, and 3.0 mg/kg, Fiduxosin blocks prostatic intraurethral pressure (IUP) responses to a greater extent than MAP responses. The effective dose (ED50) for IUP is calculated to be 0.24 mg/kg[1].
Synonyms A 185980.1, ABT 980
Molecular Weight 555.65
Formula C30H29N5O4S
CAS No. 208993-54-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Brune ME, et al. Effect of fiduxosin, an antagonist selective for alpha(1A)- and alpha(1D)-adrenoceptors, on intraurethral and arterial pressure responses in conscious dogs. J Pharmacol Exp Ther. 2002 Feb;300(2):487-94. 2. Hancock AA, et al. Preclinical pharmacology of fiduxosin, a novel alpha(1)-adrenoceptor antagonist with uroselective properties. J Pharmacol Exp Ther. 2002 Feb;300(2):478-86.

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Keywords

Fiduxosin 208993-54-8 GPCR/G Protein Neuroscience Adrenergic Receptor A 185980.1 ABT 980 inhibitor inhibit

 

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