Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate

Name	L-765,314
Synonyms	L-765314 L-765,314 Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate 1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (S)- 1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (2S)-
CAS	189349-50-6

Molecular Formula	C27H34N6O5
Molar Mass	522.6
Storage Condition	2-8°C(protect from light)
Use	L-765314 is an effective and selective antagonist of α1b adrenergic receptor (α1b adrenergic receptor), and its Ki values in rats and humans are 5.4 nM and 2.0 nM respectively.
In vitro study	L-765314 exhibits two displacement sites. The high-affinity site accounts for approximately 25% of binding (IC 50 ) 1.90 nM and represents binding to the R1b sites. The low-affinity site accounts for the residual 75% of binding (IC 50 ) 790 nM and represents binding to the R1a sites.
In vivo study	The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean C max of L-765314 (A322312) is 1.05 μM and the t 1/2 is 0.5 h. L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD 25 >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).

Last Update：2024-01-02 23:10:35

biological activity	L-765314 is a potent and selective antagonist of α1b adrenergic receptor, its Ki values in rats and humans were 5.4 nM and 2.0 nM, respectively.
Target	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).

Last Update：2024-04-09 21:54:55

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CAS: 189349-50-6
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Mobile: 18021002903
QQ: 3008007409

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Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate Request for Quotation