Tamsulosin

Name: Tamsulosin
Brand: TargetMol
SKU: T0210L
Price: 139 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.93%

货号 T0210LCas号 106133-20-4

别名 坦索罗辛, LY253351 free base, HSDB-7744, HSDB7744, HSDB 7744, Harnal-D, Flowmax, (R)-(-)-YM12617 free base

Tamsulosin ((R)-(-)-YM12617 free base) 是一种肾上腺素能受体α 1A 拮抗剂，用于良性前列腺增生(BPH)的治疗。Tansulosin 用于治疗排尿困难，这是前列腺肥大的一种常见症状。Tansulosin 和其他被称为α受体阻滞剂的药物通过放松膀胱颈部肌肉和前列腺本身的肌肉纤维来发挥作用，使其更容易排尿。

Tamsulosin

一键复制产品信息

很棒

纯度: 99.93%

货号 T0210L 别名 坦索罗辛, LY253351 free base, HSDB-7744, HSDB7744, HSDB 7744, Harnal-D, Flowmax, (R)-(-)-YM12617 free baseCas号 106133-20-4

规格	价格	库存
5 mg	¥ 139	现货
10 mg	¥ 189	现货
25 mg	¥ 313	现货
50 mg	¥ 446	现货
1 mL x 10 mM (in DMSO)	¥ 153	现货

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纯度: 99.93%

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产品介绍

Tamsulosin AI Summary

Tamsulosin is a highly potent compound with significant binding affinity across multiple adrenergic receptor subtypes. It displays exceptionally low Ki values for human Alpha-1A (0.029 nM), Alpha-1B (0.61 nM), and Alpha-1D (0.058 nM) receptors, suggesting high potency. It also shows noteworthy affinities for Alpha-2A (13.4 nM) and Alpha-2C (7.9 nM) receptors, along with rat Alpha-2B adrenergic receptor (6.8 nM). In various assays, Tamsulosin demonstrated powerful in vitro antagonism, particularly against human Alpha-1A, Alpha-1B, and Alpha-1D adrenergic receptors with further confirmation of its in vivo efficacy in an intraurethral pressure model in aged anesthetized dogs (Kd = 1.349 nM) and a spontaneously hypertensive rat model (pED50 = 7.33). The compound also exhibited inhibition of A61603-induced contraction in rats with an AD50 of 3.0 µg/kg, maintaining efficacy over 3.5 hours. Furthermore, Tamsulosin showed high affinity for human cloned Alpha-1A, Alpha-1B, and Alpha-1D receptors, with Ki values of 0.19 nM, 2.0 nM, and 0.2 nM, respectively. In pharmacokinetic evaluations, Tamsulosin displayed high oral bioavailability (Fa = 1.0), efficient evasion of hepatic elimination (Fh = 0.98), and moderate clearance rates (CL = 0.62 mL/min/kg). It exhibited a half-life of 6.8 hours in humans post-intravenous administration and a low fraction unbound (Fu = 0.01), with a steady-state volume of distribution (Vdss) of 0.21 L/kg, indicating extensive distribution across body tissues. Notably, there was no evidence of liver toxicity (DILI severity class of 0.0). Moreover, Tamsulosin possesses antagonistic activity on Alpha-1A, Alpha-1B, and Alpha-1D adrenoceptors, which is demonstrated through various IC50 values, supporting its potential in modulating adrenergic signaling pathways. In antiviral assessments, although weak against SARS-CoV-2 (hit score 0.1193), it showed 22.04% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM concentration. The compound also illustrated a degree of enzymatic inhibition, targeting human HDAC6 and MAOA, among other enzymes. These collective pharmacological characteristics suggest Tamsulosin as a promising candidate for therapeutic applications involving adrenergic receptor modulation, with a broad spectrum of potential bioactivities..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述

Tamsulosin ((R)-(-)-YM12617 free base) is an alpha1A adrenergic receptor antagonist for the symptomatic treatment of benign prostatic hyperplasia (BPH). Tamsulosin is used to treat difficulty urinating, a common symptom of an enlarged prostate. Tansulosin and other drugs called alpha blockers work by relaxing the neck muscles of the bladder and muscle fibers in the prostate itself, making it easier to urinate.

别名

坦索罗辛, LY253351 free base, HSDB-7744, HSDB7744, HSDB 7744, Harnal-D, Flowmax, (R)-(-)-YM12617 free base

化学信息

分子量	408.51
分子式	C₂₀H₂₈N₂O₅S
CAS No.	106133-20-4
Smiles	CCOc1ccccc1OCCN[C@H](C)Cc1ccc(OC)c(c1)S(N)(=O)=O
密度	1.191 g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 90 mg/mL (220.31 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (8.08 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4479 mL	12.2396 mL	24.4792 mL	122.3960 mL
5 mM	0.4896 mL	2.4479 mL	4.8958 mL	24.4792 mL
10 mM	0.2448 mL	1.2240 mL	2.4479 mL	12.2396 mL
20 mM	0.1224 mL	0.6120 mL	1.2240 mL	6.1198 mL
50 mM	0.0490 mL	0.2448 mL	0.4896 mL	2.4479 mL
100 mM	0.0245 mL	0.1224 mL	0.2448 mL	1.2240 mL