| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: =99.6%
Brimonidine (UK 14304 and AGN190342) is a highly potent and 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 reduces the progressive loss of ganglion cells to 26% and 15% at doses of 0.5 mg/kg and 1 mg/kg, respectively. In order to stop additional ganglion cell loss, brimonidine therapy is started 10 days following an increase in IOP. In ocular hypertensive retinas, brimonidine reduces the rise in GFAP immunoreactivity.
| Targets |
α adrenergic receptor
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| Enzyme Assay |
[3H]A complete agonist at alpha 2-adrenergic receptors is rimonidine (UK 14304). [3H] In the human brain, brimonidine (UK 14304) labels at least two distinct binding sites that share traits with alpha 2-adrenergic binding sites. At these two sites, GTP inhibits agonist binding, albeit to varying degrees depending on the site.
|
||
| Animal Protocol |
|
||
| References |
|
| Molecular Formula |
C11H10BRN5
|
|
|---|---|---|
| Molecular Weight |
292.14
|
|
| Exact Mass |
291.01
|
|
| Elemental Analysis |
C, 45.23; H, 3.45; Br, 27.35; N, 23.97
|
|
| CAS # |
59803-98-4
|
|
| Related CAS # |
Brimonidine tartrate; 70359-46-5; Brimonidine-d4; 1184971-51-4
|
|
| Appearance |
Solid powder
|
|
| SMILES |
C1CN=C(N1)NC2=C(C3=NC=CN=C3C=C2)Br
|
|
| InChi Key |
XYLJNLCSTIOKRM-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C11H10BrN5/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h1-4H,5-6H2,(H2,15,16,17)
|
|
| Chemical Name |
5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)quinoxalin-6-amine
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (8.56 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4230 mL | 17.1151 mL | 34.2302 mL | |
| 5 mM | 0.6846 mL | 3.4230 mL | 6.8460 mL | |
| 10 mM | 0.3423 mL | 1.7115 mL | 3.4230 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05656027 | Active Recruiting |
Drug: Brimonidine Drug: Aceclidine |
Presbyopia Miosis |
LENZ Therapeutics, Inc | December 19, 2022 | Phase 3 |
| NCT05728944 | Active Recruiting |
Drug: Aceclidine Drug: Vehicle |
Presbyopia Miosis |
LENZ Therapeutics, Inc | April 24, 2023 | Phase 3 |
| NCT05753189 | Active Recruiting |
Drug: Aceclidine Ophthalmic Solution Drug: Placebo |
Presbyopia Miosis |
LENZ Therapeutics, Inc | February 21, 2023 | Phase 3 |
| NCT05480098 | Active Recruiting |
Drug: Brimonidine Topical | Ectropion Entropion |
University of Louisville | May 26, 2022 | Phase 4 |
| NCT02039765 | Completed | Drug: Brimonidine tartrate | Hyperemia | Bausch & Lomb Incorporated | February 2014 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA