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Brimonidine tartrate

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Chemical Structure| 70359-46-5 同义名 : AGN190342 tartrate;UK 14304 tartrate;Alphagan P;AGN 190342LF;Brimonidine (tartrate);UK 1434 Tartrate
CAS号 : 70359-46-5
货号 : A139688
分子式 : C15H16BrN5O6
纯度 : 98%
分子量 : 442.221
MDL号 : MFCD07773072
存储条件:

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(113.07 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(56.53 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Brimonidine tartrate is a α2 adrenergic agonist and hydrophilic drug used for treatment of glaucoma. BRT-loaded (Brimonidine Tartarate) proniosomal gels showed an improved ocular bioavailability and sustained drug release from the prepared vesicles[3]. Clinical trials have demonstrated that brimonidine tartrate provided significantly greater efficacy, compared to vehicle, for the treatment of moderate to severe erythema of rosacea[4]. At a concentration of 0.1 µM or higher, brimonidine increased survival of purified rat RGCs (retinal ganglion cells) in the presence of glutamate neurotoxicity, oxidative stress, and hypoxia [5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.31mL

2.26mL

1.13mL

22.61mL

4.52mL

2.26mL

参考文献

[1]Gao H, Qiao X, et al. Up-regulation of brain-derived neurotrophic factor expression by brimonidine in rat retinal ganglion cells. Arch Ophthalmol. 2002 Jun;120(6):797-803.

[2]Gao H, et al. Arch Ophthalmol, 2002, 120(6), 797-803.

[3]Emad Eldeeb A, Salah S, Ghorab M. Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study. Drug Deliv. 2019 Dec;26(1):509-521. doi: 10.1080/10717544.2019.1609622. PMID: 31090464; PMCID: PMC6534210.

[4]Jackson JM, Knuckles M, Minni JP, Johnson SM, Belasco KT. The role of brimonidine tartrate gel in the treatment of rosacea. Clin Cosmet Investig Dermatol. 2015 Oct 23;8:529-38. doi: 10.2147/CCID.S58920. PMID: 26566370; PMCID: PMC4627400.

[5]Lee KY, Nakayama M, Aihara M, Chen YN, Araie M. Brimonidine is neuroprotective against glutamate-induced neurotoxicity, oxidative stress, and hypoxia in purified rat retinal ganglion cells. Mol Vis. 2010 Feb 17;16:246-51. PMID: 20161817; PMCID: PMC2822551.