L-765,314
- Product Name
- L-765,314
- CAS No.
- 189349-50-6
- Chemical Name
- L-765,314
- Synonyms
- L-765314 ，S0862;L-765314, 10 mM in DMSO;Adrenergic Receptor,L-765314,Inhibitor,Beta Receptor,L765314,inhibit,L 765314;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)-
- CBNumber
- CB22642473
- Molecular Formula
- C27H34N6O5
- Formula Weight
- 522.6
- MOL File
- 189349-50-6.mol
L-765,314 Property
- 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
N-Bromosuccinimide Price
- Product number
- CS-0021271
- Product name
- L-765314
- Purity
- 99.77%
- Packaging
- 5mg
- Price
- $110
- Updated
- 2021/12/16
- Product number
- CS-0021271
- Product name
- L-765314
- Purity
- 99.77%
- Packaging
- 10mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-0021271
- Product name
- L-765314
- Purity
- 99.77%
- Packaging
- 25mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0021271
- Product name
- L-765314
- Purity
- 99.77%
- Packaging
- 50mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0021271
- Product name
- L-765314
- Purity
- 99.77%
- Packaging
- 100mg
- Price
- $950
- Updated
- 2021/12/16
L-765,314 Chemical Properties,Usage,Production
Uses
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.
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.
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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).
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. DOI:10.1021/jm980053f
[2] Tobias B?hmer, 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. DOI:10.1111/bph.12743
L-765,314 Preparation Products And Raw materials
Raw materials
Preparation Products
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