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酒石酸溴莫尼定 /Brimonidine tartrate {[allProObj[0].p_purity_real_show]}

货号:A139688 同义名: AGN190342 tartrate;UK 14304 tartrate

Brimonidine tartrate is an α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, used to treat glaucoma through a dual mechanism of action by reducing aqueous humor production and increasing uveoscleral outflow.

Brimonidine tartrate 化学结构 CAS号:70359-46-5
Brimonidine tartrate 化学结构
CAS号:70359-46-5
Brimonidine tartrate 3D分子结构
CAS号:70359-46-5
Brimonidine tartrate 化学结构 CAS号:70359-46-5
Brimonidine tartrate 3D分子结构 CAS号:70359-46-5
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Brimonidine tartrate 纯度/质量文件 产品仅供科研

货号:A139688 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Adrenergic Receptor α-adrenergic receptor β-adrenergic receptor 其他靶点 纯度
Ivabradine HCl 98%
Maprotiline hydrochloride 98%
Cisatracurium besylate 98%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2A-adrenergic receptor, pKi: 8.9

α2B-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine HCl 98%
Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

97%
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Doxazosin mesylate 98%
Tolazoline HCl 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Brimonidine tartrate 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].

Brimonidine tartrate 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.

Brimonidine tartrate 实验方案

计算器
存储液制备 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

Brimonidine tartrate 技术信息

CAS号70359-46-5
分子式C15H16BrN5O6
分子量 442.221
别名 AGN190342 tartrate;UK 14304 tartrate;Alphagan P;AGN 190342LF;Brimonidine (tartrate);UK 1434 Tartrate
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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

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