Talinolol

Name: Talinolol
Brand: TargetMol
SKU: T21640
Price: 196 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 98.8%

货号 T21640Cas号 57460-41-0

别名 他林洛尔

Talinolol 是一种长效、心脏选择性的 β1-肾上腺素能受体阻滞剂，具有心脏保护和抗高血压作用。它也是众所周知且经常使用的 P-糖蛋白 (P-gp) 活性探针底物。

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Talinolol

一键复制产品信息

很棒

纯度: 98.8%

货号 T21640 别名 他林洛尔Cas号 57460-41-0

规格	价格	库存
1 mg	¥ 196	现货
5 mg	¥ 455	现货
10 mg	¥ 859	现货
25 mg	¥ 1,880	现货
50 mg	¥ 3,290	现货
100 mg	¥ 4,730	现货
200 mg	¥ 6,590	现货
1 mL x 10 mM (in DMSO)	¥ 490	现货

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产品介绍

Talinolol AI Summary

Talinolol exhibits diverse pharmacokinetic and bioactivity profiles across multiple experimental studies. It demonstrates toxicity in mice with LD50 values ranging from 25.0 to 1048.5 mg/kg through both intravenous and oral administration. In humans, it shows a total body clearance of 4.9 mL/min/kg and a renal clearance of 2.6 mL/min/kg, indicating renal filtration as a major elimination pathway. The hepatic clearance (CL) is recorded at 2.3 mL/min/kg, with a volume of distribution at steady state (Vdss) of 3.3 L/kg. Oral bioavailability (F_fraction) is 0.55, and the fraction absorbed (Fa) is 0.65. Talinolol exhibits notable beta-blocking activity with an activity level of 8.96 and is involved in inhibiting various targets, including the malarial parasite plastid, Glutaminase (GLS), and human tyrosyl-DNA phosphodiesterase 1 (TDP1). It inhibits the β1 and β2 adrenergic receptors with Ki values of 240.0 nM and 900.0 nM, respectively, and shows significant activity against the SARS-CoV-2 virus by inhibiting cytotoxicity in both Caco-2 and VERO-6 cells. Additionally, the compound has a high efflux ratio in human Caco2 cells, indicating active efflux transport mechanisms, and displays moderate permeability from the basolateral to apical side, with an efflux ratio indicating significant interactions with transporters. The compound shows an unbound fraction in human plasma of 0.39 and demonstrates binding affinity to various targets, including β1 adrenergic receptors and soluble epoxide hydrolase. Overall, these bioactivities and pharmacokinetic properties suggest that Talinolol has potential for further pharmacological exploration, especially in the context of its beta-blocking capabilities and antiviral activity..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	(±)-Talinolol is a selective β1 adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity.
别名	他林洛尔

化学信息

分子量	363.49
分子式	C₂₀H₃₃N₃O₃
CAS No.	57460-41-0
Smiles	CC(C)(C)NCC(O)COC1=CC=C(NC(=O)NC2CCCCC2)C=C1
密度	1.11 g/cm3 (Predicted)

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: 14 mg/mL (38.52 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7511 mL	13.7555 mL	27.5111 mL	137.5554 mL
5 mM	0.5502 mL	2.7511 mL	5.5022 mL	27.5111 mL
10 mM	0.2751 mL	1.3756 mL	2.7511 mL	13.7555 mL
20 mM	0.1376 mL	0.6878 mL	1.3756 mL	6.8778 mL