Product Details
| Product Name:
Fiduxosin |
CAS No.:
208993-54-8 |
| Purity:
99.73% |
Supply Ability:
10g |
| Release date:
2024/11/20 |
Product Introduction
Bioactivity
| Name | Fiduxosin |
| 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. |
| 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]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Keywords | Fiduxosin |
| Inhibitors Related | Octopamine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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