Brimonidine
Based on 7 publication(s) in Google Scholar
Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 59803-98-4
- Formula: C11H10BrN5
- Molecular Weight:292.13
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Brimonidine
More- Nat Biomed Eng. 2025 Sep;9(9):1547-1556. [Abstract]
- Cell Rep. 2019 Dec 3;29(10):2929-2935.e4 [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Int J Pharm. 2022 Feb 5:613:121361. [Abstract]
- J Ocul Pharmacol Ther. 2025 Sep 18. [Abstract]
- J Ocul Pharmacol Ther. 2023 Sep;39(7):456-462. [Abstract]
- J Evol Biochem Physiol. 2025 Dec 19;61(6):1706-1719.
All Adrenergic Receptor Isoforms
More
Biological Activity
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α adrenergic receptor |
[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[1][2][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 59803-98-4
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Appearance Solid
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Molecular Weight 292.13
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Formula C11H10BrN5
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Color Light yellow to yellow
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SMILES
BrC1=C2N=CC=NC2=CC=C1NC3=NCCN3
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Synonyms
UK 14304; AGN190342
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Biomed Eng
A live bacteria enzyme assay for identification of human disease mutations and drug screening. [Abstract]2025 Sep;9(9):1547-1556. PMID: 40307426 -
Cell Rep
2019 Dec 3;29(10):2929-2935.e4 PMID: 31801060 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Int J Pharm
Ocular metabolism and distribution of drugs in the rabbit eye: Quantitative assessment after intracameral and intravitreal administrations. [Abstract]2022 Feb 5:613:121361. PMID: 34896561 -
J Ocul Pharmacol Ther
Brimonidine Topical Eye Drops and Intravitreal Administration Inhibit Form-Deprivation Myopia in Guinea Pigs: Ocular Pharmacokinetics and Irritation. [Abstract]2025 Sep 18. PMID: 40966130 -
J Ocul Pharmacol Ther
Ocular Posterior Segment Distribution and Pharmacokinetics of Brimonidine After Intravitreal Administration in Guinea Pigs. [Abstract]2023 Sep;39(7):456-462. PMID: 37311153 -
Solvent & Solubility
DMSO : 50 mg/mL (171.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Andorn, A.C., M.A. Carlson, and R.C. Gilkeson, Specific [3H]UK 14,304 binding in human cortex occurs at multiple high affinity states with alpha 2-adrenergic selectivity and differing affinities for GTP. Life Sci, 1988. 43(22): p. 1805-12. [Content Brief]
[2]. Cambridge, D., UK-14,304, a potent and selective alpha2-agonist for the characterisation of alpha-adrenoceptor subtypes. Eur J Pharmacol, 1981. 72(4): p. 413-5. [Content Brief]
[3]. Chopin, P., F.C. Colpaert, and M. Marien, Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal pathway. J Pharmacol Exp Ther, 1999. 288(2): p. 798-804. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4231 mL | 17.1157 mL | 34.2313 mL | 85.5783 mL |
| 5 mM | 0.6846 mL | 3.4231 mL | 6.8463 mL | 17.1157 mL | |
| 10 mM | 0.3423 mL | 1.7116 mL | 3.4231 mL | 8.5578 mL | |
| 15 mM | 0.2282 mL | 1.1410 mL | 2.2821 mL | 5.7052 mL | |
| 20 mM | 0.1712 mL | 0.8558 mL | 1.7116 mL | 4.2789 mL | |
| 25 mM | 0.1369 mL | 0.6846 mL | 1.3693 mL | 3.4231 mL | |
| 30 mM | 0.1141 mL | 0.5705 mL | 1.1410 mL | 2.8526 mL | |
| 40 mM | 0.0856 mL | 0.4279 mL | 0.8558 mL | 2.1395 mL | |
| 50 mM | 0.0685 mL | 0.3423 mL | 0.6846 mL | 1.7116 mL | |
| 60 mM | 0.0571 mL | 0.2853 mL | 0.5705 mL | 1.4263 mL | |
| 80 mM | 0.0428 mL | 0.2139 mL | 0.4279 mL | 1.0697 mL | |
| 100 mM | 0.0342 mL | 0.1712 mL | 0.3423 mL | 0.8558 mL |