• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *