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Brimonidine Tartrate Adrenergic Receptor agonist

Name: Brimonidine Tartrate
Brand: Selleck Chemicals
SKU: S4266
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4266

Brimonidine Tartrate(UK 1434 Tartrate) is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.

Chemical Structure

Molecular Weight: 442.22

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Quality Control

Batch: Purity: 99.92%

99.92

Related Targets	CXCR Hedgehog/Smoothened PKA AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas GPR
Other Adrenergic Receptor Inhibitors	Zenidolol (ICI-118551) Hydrochloride L755507 Yohimbine HCl Atipamezole Higenamine hydrochloride Detomidine HCl Naftopidil Demethyl-Coclaurine Buflomedil HCl Fenoterol hydrobromide

Solubility

In vitro
Batch:

DMSO : 88 mg/mL (198.99 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 22 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% 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	442.22	Formula	C₁₅H₁₆BrN₅O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	70359-46-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	UK 1434 Tartrate			Smiles	C1CN=C(N1)NC2=C(C3=NC=CN=C3C=C2)Br.C(C(C(=O)O)O)(C(=O)O)O

Mechanism of Action

Targets/IC₅₀/Ki	α2a-adrenergic receptor 0.45 nM(EC50)
In vitro	Brimonidine reduces the progressive loss of ganglion cells to 26% and 15% at doses of 0.5 mg/kg and 1 mg/kg, respectively. Brimonidine administration initiates 10 days after IOP elevation prevents any further loss of ganglion cells. Brimonidine attenuates the increase in immunoreactivity of GFAP in ocular hypertensive retinas. Brimonidine, but not timolol, shows significant protection of retinal ganglion cells when applied at the time of intraocular pressure (IOP) elevation and prevents further cell loss when applied after intraocular pressure (IOP) is elevated. Brimonidine injected intravitreally into Sprague-Dawley rat eyes increases the number of BDNF-positive RGCs from 55% to 166%. Brimonidine 0.5% given as one drop before, after, or both before and after 360 degrees argon laser trabeculoplasty significantly lowers the incidence of postlaser IOP spikes. Brimonidine 0.2% instilled twice daily offers long-term IOP control comparable with that achieved with timolol 0.5% and better than betatolol 0.25% suspension.
In vivo	Brimonidine (1 mg/kg) significantly protects RGCs from elevated IOP-induced cell death in adult rats. Brimonidine (0.0001%) BMD results in the loss of approximately 37% of the retinal ganglion cell (RGC) population and has no significant neuroprotective effects in adult Sprague-Dawley rats. Brimonidine (0.001% or 0.01%) results in the survival of 76 or 90%, respectively, of the RGC population, and 0.1% Brimonidine fully prevents retinal ganglion cell (RGC) death in the first 7 days after ischemia in adult Sprague-Dawley rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11687528/ [2] https://pubmed.ncbi.nlm.nih.gov/12049586/ [3] https://pubmed.ncbi.nlm.nih.gov/9264305/ [4] https://pubmed.ncbi.nlm.nih.gov/11549376/ [5] https://pubmed.ncbi.nlm.nih.gov/11950228/

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