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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 59803-98-4 Chemical Structure| 59803-98-4

Structure of Brimonidine
CAS No.: 59803-98-4

Chemical Structure| 59803-98-4

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UK-14304 is an adrenergic receptor α2 agonist which can activate ERK in epicardial coronary artery culture, inhibit R-type calcium currents, as well as inhibit hormone-sensitive lipase activity and suppresses lipogenesis in adipose tissue.

Synonyms: AGN190342; UK-14304; Alphagan P

4.5 *For Research Use Only !

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Product Details of Brimonidine

CAS No. :59803-98-4
Formula : C11H10BrN5
M.W : 292.13
SMILES Code : BrC1=C2N=CC=NC2=CC=C1NC3=NCCN3
Synonyms :
AGN190342; UK-14304; Alphagan P
MDL No. :MFCD00153878
InChI Key :XYLJNLCSTIOKRM-UHFFFAOYSA-N
Pubchem ID :2435

Safety of Brimonidine

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P264-P270-P301+P310+P330-P405-P501
Class:6.1
UN#:2811
Packing Group:

Related Pathways of Brimonidine

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human trabecular meshwork (HTM) cells 10 μM 6 days To investigate the effects of Brimonidine on the metabolic function of TGF-β2-treated HTM cells, results showed that Brimonidine canceled the TGF-β2-induced reduction in maximal mitochondrial respiration but had no effect on glycolytic capacity. Bioengineering (Basel). 2022 Jul 12;9(7):310
rat retinal rod bipolar cells 0.1, 0.3, 1 μM To investigate the inhibitory effect of Brimonidine on presynaptic Ca2+ signals in rod bipolar cells J Neurosci. 2014 Jul 9;34(28):9432-40
Müller glia 1 μM 3, 6, 12, 24 h BMD significantly increased mRNA expression levels of NGF, BDNF, and bFGF, but not NT-3, CNTF, or GDNF. Cell Death Dis. 2014 Jul 17;5(7):e1341

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Microbead-induced ocular hypertensive model Topical eye drop 0.15% Twice daily for 2 weeks To evaluate the IOP-lowering effect of Brimonidine and its protective effects on retinal ganglion cells and axons in the microbead-induced ocular hypertensive mouse model. Results showed that Brimonidine significantly reduced IOP and improved the survival of retinal ganglion cells and axons. Invest Ophthalmol Vis Sci. 2012 Jun 20;53(7):3733-41
Brown Norway rats Retinal ischemia and glaucoma models Eyedrops 0.6 μM To investigate the neuroprotective effect of Brimonidine on retinal ganglion cells J Neurosci. 2014 Jul 9;34(28):9432-40
New Zealand white rabbits Normotensive rabbit model Supraciliary space injection 1.5 µg, 0.75 µg, 0.015 µg Single injection, lasting 9 hours To evaluate the effect of Brimonidine on reducing intraocular pressure via supraciliary space injection. Results showed that a dose of 1.5 μg reduced IOP by approximately 3.3 mmHg within 1 hour, and the effect lasted for about 9 hours. Invest Ophthalmol Vis Sci. 2014 Sep 11;55(11):7387-97
Mice Optic nerve injury model Eye drops 1.0% Once daily for 2 weeks Brimonidine promotes optic nerve regeneration by inducing Erk1/2 phosphorylation and upregulating TrkB expression while downregulating p75 expression. Cell Death Dis. 2013 Aug 8;4(8):e763
Mice EAAC1-deficient mice Topical eye drops 1.0% BMD Once daily from 5 weeks to 8 weeks of age BMD significantly protected RGCs in EAAC1 KO mice, reduced thinning of the inner retinal layer, and improved visual function. BMD also suppressed NR2B phosphorylation, reducing excitotoxicity. Cell Death Dis. 2014 Jul 17;5(7):e1341
Rats Elevated intraocular pressure model Subcutaneous injection 1 mg/kg Once daily for 8 weeks Brimonidine significantly improved retinal ganglion cell survival, particularly in the nasal region of the retina. Brimonidine treatment also preserved ganglion cell axon morphology, sampling density and total number in the optic nerve. Additionally, brimonidine significantly reduced the deficits in axonal transport associated with elevated ocular pressure. Mol Neurodegener. 2011 Jan 13;6(1):4

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02249065 Rosacea PHASE4 COMPLETED 2025-08-15 Johnson Dermatology, Fort Smit... More >>h, Arkansas, 72916, United States|Blue Harbor Dermatology, Newport Beach, California, 92663, United States|Center for Dermatology and Laser Surgery, Sacramento, California, 95819, United States|Redwood Dermatology Research, Santa Rosa, California, 95403, United States|Florida Academic Dermatology Center, Miami, Florida, 33136, United States|Research Institute of the Southeast, West Palm Beach, Florida, 33401, United States|Grekin Skin Institute, Warren, Michigan, 48088, United States|Advanced Skin Research Center, Omaha, Nebraska, 68144, United States|Manhattan Dermatology and Cosmetic Surgery, New York, New York, 10017, United States|DermDox Centers for Dermatology, Hazleton, Pennsylvania, 18201, United States|Arlington Research Center, Arlington, Texas, 76011, United States|Texas Dermatology and Laser Specialists, San Antonio, Texas, 78218, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.12mL

3.42mL

1.71mL

34.23mL

6.85mL

3.42mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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