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L-765314

Catalog No. T5511   CAS 189349-50-6

L-765314 is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B. It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure.

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L-765314 Chemical Structure
L-765314, CAS 189349-50-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 40.00
2 mg In stock $ 57.00
5 mg In stock $ 89.00
10 mg In stock $ 147.00
25 mg In stock $ 287.00
50 mg In stock $ 455.00
100 mg In stock $ 672.00
1 mL * 10 mM (in DMSO) In stock $ 97.00
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Purity: 99.95%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description L-765314 is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B. It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure.
Targets&IC50 α1B-adrenoceptor:2.0 nM (ki) human, α1B-adrenoceptor:5.4 nM(ki) rat
In vivo 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)[1]
Molecular Weight 522.6
Formula C27H34N6O5
CAS No. 189349-50-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (95.68 mM), Sonification is recommended.

TargetMolReferences and Literature

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. Kim J , Kim Y H , Bang S , et al. L-765,314 Suppresses Melanin Synthesis by Regulating Tyrosinase Activity[J]. Molecules, 2019, 24(4). 3. 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.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Compound Library Neurotransmitter Receptor Compound Library Endocrinology-Hormone Compound Library Bioactive Compounds Library Max Anti-Alzheimer's Disease Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library

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Keywords

L-765314 189349-50-6 GPCR/G Protein Neuroscience Adrenergic Receptor L 765314 Inhibitor Beta Receptor L765314 inhibit inhibitor

 

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