GlpBio

L-765314

目录号: GC32670纯度: >99.50%
L-765314 is a selective and potent α1b-adrenoceptor (α1b adrenergic receptor) antagonist with an IC50 of 1.90 nM and Kis of 5.4 and 2.0 for rat and human α1b adrenergic receptor, respectively.
L-765314
Cas No.: 189349-50-6
规格价格库存数量操作
5mg¥495.00现货
1
10mg¥765.00现货
1
25mg¥1,530.00现货
1
50mg¥2,430.00现货
1
100mg¥3,600.00现货
1
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产品描述 Description

L-765314 is a selective and potent α1b-adrenoceptor (α1b adrenergic receptor) antagonist with an IC50 of 1.90 nM and Kis of 5.4 and 2.0 for rat and human α1b adrenergic receptor, respectively.

L-765,314 is a potent and selective α1b adrenergic receptor antagonist, which also reduces melanin production by targeting the protein kinase C (PKC)-dependent regulation of tyrosinase activity and raises the intracellular level of melanin precursors.[2]

[1] Patane MA, et al. Journal of Medicinal Chemistry, 41(8), 1205–1208. [2] Kim J, et al. Molecules. 2019 Feb 21;24(4):773.

实验参考方法 Experimental Reference Method

Animal experiment:

Rats[1]The potency of terazosin and L-765314 for inhibiting the pressor responses to phenylephrine and A-61603 is evaluated in anesthetized male Sprague-Dawley rats (n=4). The rats are dosed i.v with either vehicle or ascending doses of test compounds, and the peak changes in mean arterial pressure are measured. The dose of antagonist eliciting a 25 mmHg decrease in mean arterial pressure (AD25) is calculated as an index of hypotensive potency. The rats are dosed i.v with L-765314 at 3 mg/kg , and the plasma is assayed by LCMS for parent compound[1].

References:

[1]. Patane MA, et al. 4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist. J Med Chem. 1998 Apr 9;41(8):1205-8.
[2]. Tobias Böhmer, et al. The α1B-adrenoceptor subtype mediates adrenergic vasoconstriction in mouse retinal arterioles with damaged endothelium. Br J Pharmacol. 2014 Aug; 171(16): 3858–3867.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
189349-50-6
SMILES
O=C(N1[C@H](C(NC(C)(C)C)=O)CN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)OCC4=CC=CC=C4
分子式
C27H34N6O5
分子量
522.6 g/mol
溶解性
DMSO : 50 mg/mL (95.68 mM; Need ultrasonic)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol