Fiduxosin
Fiduxosin is a potent α1-adrenoceptor antagonist, with Ki of 0.160 nM, 24.9 nM, and 0.920 nM for α1a-, α1b-, and α1d-adrenoceptors, respectively.
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- CAS No.: 208993-54-8
- 화학식: C30H29N5O4S
- 분자량:555.65
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Adrenergic Receptor Isoforms
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Biological Activity
제품 설명
IC50 & Target
Ki: 0.16 nM (α1a-adrenoceptor), 24.9 nM (α1b- adrenoceptor), 0.92 nM (α1d-adrenoceptor), 92 nM (Human α2a-adrenoceptor), 22 nM (Human α2c-adrenoceptor), 21 nM (Rat α2b-adrenoceptor), 29 nM (Rat 5HT1A receptor)[1]
In Vitro
Fiduxosin displays low affinity for other adrenoceptors, including cloned human α2a- (92 nM) and α2c-adrenoceptors (22 nM) and rat neonatal lung α2b-adrenoceptors (21 nM), in addition to β-adrenoceptors (2-5 μM). Fiduxosin also has low affinity for 5HT1A receptors in rat cortex (29 nM) compared with its affinity at α1a-adrenoceptors (0.16 nM). Fiduxosin antagonizes competitively PE-induced responses with a pA2 value of 7.58, in the rabbit urethra[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 208993-54-8
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분자량 555.65
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화학식 C30H29N5O4S
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SMILES
O=C(N1CCCCN2C[C@]3([H])[C@](COC4=CC=CC(OC)=C34)([H])C2)C5=C(NC1=O)C6=NC(C7=CC=CC=C7)=CN=C6S5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. 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. [Content Brief]
[2]. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fiduxosin Related Classifications
HY-U00399 Related Classifications
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