Home GPCR & G Protein Adrenergic Receptor agonist Brimonidine Tartrate For research use only.

Brimonidine Tartrate

Synonyms: UK 1434 Tartrate

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.

Brimonidine Tartrate Chemical Structure

Brimonidine Tartrate Chemical Structure

CAS: 70359-46-5

Purity & Quality Control

Batch: Purity: 99.92%
99.92

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Biological Activity

Description 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.
Targets
α2a-adrenergic receptor [1]
0.45 nM(EC50)
In vitro
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. [1] Brimonidine injected intravitreally into Sprague-Dawley rat eyes increases the number of BDNF-positive RGCs from 55% to 166%. [2] 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. [3]
In Vivo
In vivo

Brimonidine (1 mg/kg) significantly protects RGCs from elevated IOP-induced cell death in adult rats. [4] 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. [5]

Chemical lnformation & Solubility

Molecular Weight 442.22 Formula

C15H16BrN5O6
CAS No. 70359-46-5 SDF Download Brimonidine Tartrate SDF
Smiles C1CN=C(N1)NC2=C(C3=NC=CN=C3C=C2)Br.C(C(C(=O)O)O)(C(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 88 mg/mL ( (198.99 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 22 mg/mL

Ethanol : Insoluble


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In vivo
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