Home GPCR & G Protein Adrenergic Receptor agonist Brimonidine Tartrate

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Brimonidine Tartrate Adrenergic Receptor agonist

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.
Brimonidine Tartrate Adrenergic Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 442.22

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Quality Control

Batch: Purity: 99.92%
99.92

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

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 442.22 Formula

C15H16BrN5O6

 Storage (From the date of receipt)
CAS No. 70359-46-5 Download SDF Storage of Stock Solutions

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

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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
  • [4] https://pubmed.ncbi.nlm.nih.gov/11549376/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11950228/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-01)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04007276 NOT_YET_RECRUITING
Glaucoma; Glaucoma, Open-Angle; Glaucoma; Drugs; Droopy Eyelid; Ptosis; Glaucoma, Primary Open Angle
Tulane University
 2026-11-10 PHASE4
NCT07390578 NOT_YET_RECRUITING
Acquired Ptosis
Duke University
 2026-12-01 PHASE4
NCT07690397 ACTIVE_NOT_RECRUITING
Primary Open-Angle Glaucoma (POAG); Ocular Hypertension
Tecnoquimicas
 2026-06-10 PHASE4
NCT06365853 ACTIVE_NOT_RECRUITING
Recurrent Ovarian Cancer; Folate Receptor-Alpha Positive
AbbVie
 2024-07-29 PHASE2
NCT07209410 RECRUITING
Glaucoma
Insight Eyecare Specialties, Inc. dba Vision Source Eyecare,
 2025-11-01 PHASE4
NCT07082764 NOT_YET_RECRUITING
Chemotherapy Induced Peripheral Neuropathy
Tarian Pharma
 2025-09-01 PHASE2

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