L-765,314 manufacturers
- L-765314
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- $44.00 / 5mg
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2024-11-19
- CAS:189349-50-6
- Min. Order:
- Purity: 99.73%
- Supply Ability: 10g
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| | L-765,314 Basic information |
| Product Name: | L-765,314 | | Synonyms: | 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)-;Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate;Adrenergic Receptor,L-765314,Inhibitor,Beta Receptor,L765314,inhibit,L 765314 | | CAS: | 189349-50-6 | | MF: | C27H34N6O5 | | MW: | 522.6 | | EINECS: | | | Product Categories: | | | Mol File: | 189349-50-6.mol |  |
| | L-765,314 Chemical Properties |
| density | 1.269±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C(protect from light) | | solubility | DMSO:75.0(Max Conc. mg/mL);143.51(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);191.35(Max Conc. mM) | | pka | 14.99±0.20(Predicted) | | form | Solid | | color | White to off-white |
| | L-765,314 Usage And Synthesis |
| Biological Activity | L-765314 is a potent and selective antagonist of the α1b adrenergic receptor with Ki values of 5.4 nM and 2.0 nM in rat and human, respectively. | | in vitro | 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. < /div> | | in vivo | 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. It 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, it 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). | | 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). |
| | L-765,314 Preparation Products And Raw materials |
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