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    Brimonidine Tartrate (UK 14304; AGN190342)
    Brimonidine Tartrate (UK 14304; AGN190342)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1105
    CAS #: 70359-46-5Purity ≥98%

    Description: Brimonidine Tartrate (AGN-190342; UK14304; UK-14304; Alphagan), the tartrate salt of Brimonidine, is a highly potent and selective α-adrenergic receptor agonist  with anti-hypertensive effects. It activates the α2A adrenoreceptor with an EC50 of 0.45 nM. Brimonidine was approved to treat open-angle glaucoma or ocular hypertension. 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. 

    References: Invest Ophthalmol Vis Sci. 2001 Nov;42(12):2849-55; Brain Res. 2001 Sep 21;913(2):133-9.

    Related CAS#: 59803-98-4 (free base); 70359-46-5 (tartrate)    

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    Molecular Weight (MW)442.22 
    FormulaC15H16BrN5O6 
    CAS No.70359-46-5  (tartrate salt);
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 88 mg/mL (199 mM)
    Water: <1 mg/mL
    Ethanol: 75 mg/mL (169.6 mM) 
    SMILES C1CN=C(N1)NC2=C(C3=NC=CN=C3C=C2)Br.C(C(C(=O)O)O)(C(=O)O)O
    Synonyms AGN 190342; UK 14304; UK14304; Alphagan; AGN-190342; AGN190342; UK 14,304-18; UK 14,304; UK-14304; UK-14,304-18; UK-14,308


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: [3H]Brimonidine (UK 14304) is a full agonist at alpha 2-adrenergic receptors. [3H]Brimonidine (UK 14304) labels at least 2 specific binding sites in human brain that both have the characteristics of an alpha 2-adrenergic binding site. GTP decreases agonist binding at both of these sites, but with different potencies at each site.

    In VivoBrimonidine (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. 
    Animal modelRats
    Formulation & Dosage1 mg/kg
    ReferencesInvest Ophthalmol Vis Sci. 2001 Nov;42(12):2849-55; Brain Res. 2001 Sep 21;913(2):133-9. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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