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BRL 52537 hydrochloride

カタログ番号GC15313

κ/μオピオイド受容体アゴニスト、強力かつ選択的

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BRL 52537 hydrochloride 化学構造

Cas No.: 112282-24-3

サイズ 価格 在庫数 個数
5mg
$86.00
在庫あり
10mg
$135.00
在庫あり
25mg
$252.00
在庫あり
50mg
$378.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of BRL 52537 hydrochloride

BRL 52537 hydrochloride is a potent and selective agonist of κ/μ-opioid receptor with Ki value of 0.24 nM for κ-opioid receptor [1].

The κ-opioid receptor (KOR) is a type of opioid receptor for opioid peptide dynorphin and controls addiction. Also, KOR plays an important role in stress, anxiety, anhedonia, depression and increased drug-seeking behavior.

BRL 52537 hydrochloride is a potent and selective κ/μ-opioid receptor agonist. In the mouse tail flick model, BRL 52537 showed antinociception with ED50 value of 0.05 mg/kg, which was 25 times more potent than morphine [1]. In WT male mice with middle cerebral artery occlusion, BRL 52537 significantly decreased infarct volumes at 72 h of reperfusion. However, BRL 52537 had no effect in neuronal NO synthase null mutants (nNOS-/-) mice or in the WT female mice. These results suggested that BRL 52537 exhibited neuroprotection through inhibition of ischemia-evoked NO production and nNOS activity [2]. In adult rat dorsal root ganglia (DRGs), BRL 52537 inhibited tetrodotoxin-resistant (TTX-r) sodium currents in an opioid receptor-independent way, which also contributed to the antinociceptive effects [3]. In rats with cerebral ischemia/reperfusion (I/R) injury, BRL52537 inhibited neuronal apoptosis and brain damage. Also, BRL52537 increased the level of phosphorylated STAT3 and reduced caspase-3 expression [4].

References:
[1].  Vecchietti V, Giordani A, Giardina G, et al. (2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics. J Med Chem, 1991, 34(1): 397-403.
[2].  Zeynalov E, Nemoto M, Hurn PD, et al. Neuroprotective effect of selective kappa opioid receptor agonist is gender specific and linked to reduced neuronal nitric oxide. J Cereb Blood Flow Metab, 2006, 26(3): 414-420.
[3].  Su X, Castle NA, Antonio B, et al. The effect of kappa-opioid receptor agonists on tetrodotoxin-resistant sodium channels in primary sensory neurons. Anesth Analg, 2009, 109(2): 632-640.
[4].  Fang S, Xu H, Lu J, et al. Neuroprotection by the kappa-opioid receptor agonist, BRL52537, is mediated via up-regulating phosphorylated signal transducer and activator of transcription-3 in cerebral ischemia/reperfusion injury in rats. Neurochem Res, 2013, 38(11): 2305-2312.

Chemical Properties of BRL 52537 hydrochloride

Cas No. 112282-24-3 SDF
Chemical Name 2-(3,4-dichlorophenyl)-1-(2-(pyrrolidin-1-ylmethyl)piperidin-1-yl)ethanone hydrochloride
Canonical SMILES ClC1=C(Cl)C=C(CC(N2CCCCC2CN3CCCC3)=O)C=C1.Cl
Formula C18H24Cl2N2O.HCl M.Wt 391.77
溶解度 <1.96mg/ml in Water Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of BRL 52537 hydrochloride

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1 mg 5 mg 10 mg
1 mM 2.5525 mL 12.7626 mL 25.5252 mL
5 mM 0.5105 mL 2.5525 mL 5.105 mL
10 mM 0.2553 mL 1.2763 mL 2.5525 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 3 reference(s) in Google Scholar.)

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