货号	规格	价格	上海	北京	珠海	重庆	武汉
S89036-5mg	≥98%	￥350.00 S89036-5mg ￥350.00 现货	10 10	-	-	-	-
S89036-10mg	≥98%	￥540.00 S89036-10mg ￥540.00 现货	9 9	-	-	-	-
S89036-25mg	≥98%	￥1080.00 S89036-25mg ￥1080.00 现货	4 4	-	-	-	-
S89036-100mg	≥98%	￥2560.00 S89036-100mg ￥2560.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

Ki: 5.4±0.6 nM (rat α1b receptor ), 2.0±0.66 nM (human α1b receptor), 50±8 nM (rat α1d receptor), 34±6 nM (human α1d receptor), 500±20 nM (rat α1b receptor ), 420±62 nM (human α1b receptor);AdrenergicReceptor

体内研究：

The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean Cmax of L-765314 (A322312) is 1.05 μM and the t1/2 is 0.5 h. L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD25>3 mg/kg for each). On the basis of the inhibition of pressor responses to the R1a subtype selective agonist A-61603, L-765314 appears to be selective versus the R1a receptor up to a dose of 0.3 mg/kg. The results of hypotensive potency in rats show that both L-765314 and terazosin tend to decrease heart rate (about 25 bpm at 1 mg/kg iv)

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.914 ml	9.568 ml	19.135 ml
5 mM	0.383 ml	1.914 ml	3.827 ml
10 mM	0.191 ml	0.957 ml	1.914 ml
50 mM	0.038 ml	0.191 ml	0.383 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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