Guanabenz Acetate

产品说明书

Print
Chemical Structure| 23256-50-0 同义名 : Wy8678 acetate;BR-750
CAS号 : 23256-50-0
货号 : A461798
分子式 : C10H12Cl2N4O2
纯度 : 99%
分子量 : 291.134
MDL号 : MFCD00153801
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(171.74 mM),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: 2.5 mg/mL(8.59 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方:

4% DMSO+30% PEG 300+water 5 mg/mL

生物活性
描述 Guanabenz Acetate is an alpha2 adrenergic receptor agonist shown to interact with a regulatory subunit of the protein phosphatase, Pp1/Gadd34, and selectively disrupt the dephosphorylation of the alpha subunit of eukaryotic initiation factor 2.Guanabenz treatment accelerated ALS-like disease progression in a strain of mutant SOD1 transgenic ALS(Amyotrophic Lateral Sclerosis) mice[3]. Guanabenz Acetate is capable of markedly increasing the cellular internalization and target mRNA silencing of hydrophobically modified siRNAs (hsiRNAs), yielding a ∼100-fold decrease in hsiRNA IC50 (from 132 nM to 2.4 nM)[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02423083 Multiple Sclerosis, Relapsing-... 展开 >>Remitting Multiple Sclerosis 收起 << Phase 1 Terminated - United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 <<
NCT02443103 Bone Cancer M... 展开 >>etastasis 收起 << Not Applicable Terminated(Slow accrual) - United States, Indiana ... 展开 >> Indiana University Health Hospital Indianapolis, Indiana, United States, 46202 Indiana University Melvin and Bren Simon Cancer Center Indianapolis, Indiana, United States, 46202 Sidney & Lois Eskenazi Hospital Indianapolis, Indiana, United States, 46202 Spring Mill Medical Center Indianapolis, Indiana, United States, 46290 收起 <<
NCT02443103 - Terminated(Slow accrual) - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.17mL

3.43mL

1.72mL

34.35mL

6.87mL

3.43mL

参考文献

[1]Noguchi S, Jianmongkol S, et al. Guanabenz-mediated inactivation and enhanced proteolytic degradation of neuronal nitric-oxide synthase. J Biol Chem. 2000 Jan 28;275(4):2376-80.

[2]Jasper JR, Lesnick JD, et al. Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S] GTPgammaS binding. Biochem Pharmacol. 1998 Apr 1;55(7):1035-43.

[3]Vieira FG, Ping Q, Moreno AJ, Kidd JD, Thompson K, Jiang B, Lincecum JM, Wang MZ, De Zutter GS, Tassinari VR, Levine B, Hatzipetros T, Gill A, Perrin S. Guanabenz Treatment Accelerates Disease in a Mutant SOD1 Mouse Model of ALS. PLoS One. 2015 Aug 19;10(8):e0135570.

[4] Osborn MF, Alterman JF, Nikan M, Cao H, Didiot MC, Hassler MR, Coles AH, Khvorova A. Guanabenz (Wytensin™) selectively enhances uptake and efficacy of hydrophobically modified siRNAs. Nucleic Acids Res. 2015 Oct 15;43(18):8664-72.