L-765314 Adrenergic Receptor antagonist

Cat.No.S0862

L-765314 is a selective and potent α1b-adrenoceptor (α1b adrenergic receptor) antagonist with an IC50 of 1.90 nM and Kis of 5.4 and 2.0 for rat and human α1b adrenergic receptor, respectively.
L-765314 Adrenergic Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 522.60

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Quality Control

Batch: S086201 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.95%
99.95

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (191.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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%
% Tween 80
% ddH2O
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 522.60 Formula

C27H34N6O5

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 189349-50-6 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=CC2=NC(=NC(=C2C=C1OC)N)N3CCN(C(C3)C(=O)NC(C)(C)C)C(=O)OCC4=CC=CC=C4

Mechanism of Action

Targets/IC50/Ki
α1b-adrenoceptor
1.9 nM
α1b-adrenoceptor
(in receptor binding affinity to human experiment)
2 μM(Ki)
α1b-adrenoceptor
(in receptor binding affinity to rat experiment)
5.4 μM(Ki)
In vitro

L-765,314 is a potent and selective α1b adrenergic receptor antagonist, which also reduces melanin production by targeting the protein kinase C (PKC)-dependent regulation of tyrosinase activity and raises the intracellular level of melanin precursors.

References

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