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Guanabenz Acetate/氯苄氨胍醋酸盐 {[allProObj[0].p_purity_real_show]}

货号:A461798 同义名: 醋酸胍那苄 / Wy8678 acetate; BR-750

Guanabenz Acetate 是一种中枢作用的 α2-肾上腺素能受体激动剂,常用于高血压及交感神经调控机制研究。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Guanabenz Acetate/氯苄氨胍醋酸盐 化学结构 CAS号:23256-50-0
Guanabenz Acetate/氯苄氨胍醋酸盐 化学结构
CAS号:23256-50-0
Guanabenz Acetate/氯苄氨胍醋酸盐 3D分子结构
CAS号:23256-50-0
Guanabenz Acetate/氯苄氨胍醋酸盐 化学结构 CAS号:23256-50-0
Guanabenz Acetate/氯苄氨胍醋酸盐 3D分子结构 CAS号:23256-50-0
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Guanabenz Acetate/氯苄氨胍醋酸盐 纯度/质量文件 产品仅供科研

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Ivabradine HCl 98%
Maprotiline HCl 98%
Cisatracurium besylate 96%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-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%
Labetalol HCl 98+%
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

99%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Carvedilol 99%
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Tolazoline HCl 98%
Esmolol HCl 95%
Propranolol HCl ++

β-adrenergic receptor, IC50: 12 nM

99%
Zenidolol HCl ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

98%
Acebutolol HCl 97+%
Carteolol HCl 98+%
Betaxolol 99%
Betaxolol HCl +

β1-adrenergic receptor, IC50: 6 μM

97%
Bisoprolol 97%
Sotalol HCl 95+%
Nebivolol HCl +++

β1-adrenoceptor, IC50: 0.8 nM

99%
Metoprolol 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。

Guanabenz Acetate/氯苄氨胍醋酸盐 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].

Guanabenz Acetate/氯苄氨胍醋酸盐 细胞实验

Cell Line
Concentration Treated Time Description References
DLD1 cells 50 µM 48 hours GBZ treatment reduced the expression of β-catenin target genes Nat Commun. 2022 Feb 3;13(1):674.
HeLa cells 0-200 µM 24 hours To assess the impact of Guanabenz on HeLa cell viability, showing toxicity at concentrations of 125 µM and above. Nucleic Acids Res. 2015 Oct 15;43(18):8664-72.
HCM-BROD-0106-C71 cells 50 µM 24 hours To evaluate the cytotoxicity of Guanabenz on patient-derived glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on patient-derived glioblastoma cells. Neurotherapeutics. 2021 Apr;18(2):1371-1392.
T98G-R cells 50 µM 24 hours To evaluate the cytotoxicity of Guanabenz on TMZ-resistant glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on TMZ-resistant glioblastoma cells. Neurotherapeutics. 2021 Apr;18(2):1371-1392.
A172 cells 50 µM 24 hours To evaluate the cytotoxicity of Guanabenz on glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on glioblastoma cells and reduced Sunitinib-induced autophagy. Neurotherapeutics. 2021 Apr;18(2):1371-1392.
U-87MG cells 50 µM 24 hours To evaluate the cytotoxicity of Guanabenz on glioblastoma cells and its combined effect with Sunitinib. Results showed that Guanabenz enhanced the cytotoxicity of Sunitinib on glioblastoma cells and reduced Sunitinib-induced autophagy. Neurotherapeutics. 2021 Apr;18(2):1371-1392.
Human placental BeWo cell line 5 µM 24 hours To assess the effect of GADD34 inhibition on ER stress-induced reduction in mTORC1 activity, results showed that guanabenz attenuated the tunicamycin-mediated increase in CHOP protein levels and reduction in mTORC1 activity Cell Commun Signal. 2023 Nov 13;21(1):326.
SW480 cells 50 µM 48 hours GBZ treatment decreased β-catenin levels, which was markedly attenuated by conductin knockout Nat Commun. 2022 Feb 3;13(1):674.
Differentiated oligodendrocyte progenitor cells (dOPCs) 5.0 µM 48 hours Guanabenz protected dOPCs from IFN-γ-mediated apoptotic death, restoring cell survival to control levels. Nat Commun. 2015 Mar 13;6:6532.
J774.1 cells 50 µM 6 hours Measure mRNA expression levels of inflammatory cytokines, results showed that Guanabenz blocked LPS-induced increases in IFN-γ, TNF-α, IL-6, IL-1β, and COX-2 mRNA expression mBio. 2019 Apr 30;10(2):e00381-19.
Primary macrophages 10 µM 6 hours Suppressed LPS-induced upregulation of IL1β, IL6, TNFα, and Cox2 mRNA expression Int J Mol Sci. 2016 May 5;17(5):674.
RAW264.7 macrophages 10 µM 6 hours Suppressed LPS-induced upregulation of IL1β, IL6, TNFα, and Cox2 mRNA expression Int J Mol Sci. 2016 May 5;17(5):674.
Bone marrow-derived dendritic cells 50 µM 8 hours To evaluate the effect of GBZ on IL-10 production in LPS-stimulated dendritic cells. Results showed that GBZ increased IL-10 production. Front Immunol. 2017 Jun 13;8:679.
U2OS cells 50 µM Overnight GBZ treatment induced condensation of transiently expressed conductin Nat Commun. 2022 Feb 3;13(1):674.
HMC-1.1 mast cells 10 µM Suppressed PMA-induced upregulation of TNFα and IL13 mRNA expression Int J Mol Sci. 2016 May 5;17(5):674.
Jurkat T lymphocytes 5 or 10 µM Suppressed PMA-induced upregulation of IL2 and IFNγ mRNA expression Int J Mol Sci. 2016 May 5;17(5):674.

Guanabenz Acetate/氯苄氨胍醋酸盐 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice MPZmutant mice and SOD1mutant mice Oral 1 mg/kg or 5 mg/kg Twice a day or once a day for several weeks to months Sephin1 prevented the motor, morphological, and molecular defects of MPZmutant and SOD1mutant mice without adverse effects. Science. 2015 Apr 10;348(6231):239-42
NOD-SCID mice U-87MG glioblastoma xenograft model Peritumoral injection 10 mg/kg 3 injections on days 14, 21, and 28 To evaluate the therapeutic effect of combined treatment with Guanabenz and Sunitinib on glioblastoma xenograft model. Results showed that combined treatment significantly inhibited tumor growth, reduced Ki67 expression, and decreased autophagy-related markers. Neurotherapeutics. 2021 Apr;18(2):1371-1392.
BALB/cJ and C57BL/6J mice Chronic Toxoplasma infection model Oral gavage 10 mg/kg Once daily for 3 to 6 weeks Evaluate the effects of Guanabenz on brain cyst burden and neuroinflammation in chronically Toxoplasma-infected mice. Results showed that Guanabenz significantly reduced brain cyst burden (~75%) in BALB/cJ mice via i.p. injection and reversed Toxoplasma-induced hyperactivity, which correlated with reduced neuroinflammation. However, in C57BL/6J mice, Guanabenz increased cyst burden but still reversed hyperactivity. mBio. 2019 Apr 30;10(2):e00381-19.
C57BL/6 mice D-galactosamine/LPS-induced liver damage model Intraperitoneal injection 2 mg/kg Single injection, observed for 48 hours To evaluate the effect of GBZ on d-galN/LPS-induced liver damage and mortality. Results showed that GBZ significantly improved Mice survival, reduced liver damage, increased IL-10 levels, and inhibited TNF-α production. Front Immunol. 2017 Jun 13;8:679.
Drosophila OPMD model Oral 3 mM Daily administration until adulthood Alleviate OPMD phenotypes, including muscle degeneration and nuclear inclusion formation EMBO Mol Med. 2011 Jan;3(1):35-49
Mice GFAP/tTA; TRE/IFN-γ transgenic mice Intraperitoneal injection 4 mg/kg Daily from P7 to P18 Guanabenz protected oligodendrocytes and myelin from the detrimental effects of IFN-γ, restoring myelination to levels observed in wild type littermates. Nat Commun. 2015 Mar 13;6:6532.
C57BL/6 mice Tunicamycin-induced ER stress model Intraperitoneal injection 4 mg/kg For 3 consecutive days Sephin1 significantly suppressed tunicamycin-induced renal tubular cell death, improved survival, and markedly suppressed nuclear translocation of CHOP. Cell Death Dis. 2025 Feb 19;16(1):117.
C57BL/6 mice OVX-induced osteoporosis model Intraperitoneal injection 4, 8 mg/kg Every two days for 6 weeks Inhibition of OVX-induced osteoporosis Acta Pharmacol Sin. 2024 Apr;45(4):790-802.
BALB/cJ and C57BL/6J mice Chronic Toxoplasma infection model Intraperitoneal injection 5 mg/kg Once daily for 3 to 6 weeks Evaluate the effects of Guanabenz on brain cyst burden and neuroinflammation in chronically Toxoplasma-infected mice. Results showed that Guanabenz significantly reduced brain cyst burden (~75%) in BALB/cJ mice via i.p. injection and reversed Toxoplasma-induced hyperactivity, which correlated with reduced neuroinflammation. However, in C57BL/6J mice, Guanabenz increased cyst burden but still reversed hyperactivity. mBio. 2019 Apr 30;10(2):e00381-19.
BALB/c nude mice SW480 xenograft model Oral 50 µM Daily for 20 days GBZ treatment reduced tumor growth by about 60% Nat Commun. 2022 Feb 3;13(1):674.
Mice Tsc1 conditional knockout mice Intraperitoneal injection 8 mg/kg Once daily from P7 to P14 To evaluate the effect of Guanabenz on oligodendrocyte survival and myelination in Tsc1 mutant mice, results showed that Guanabenz treatment partially rescued myelination defects Nat Commun. 2016 Jul 15;7:12185
Mice (C57BL/6J) Experimental autoimmune encephalomyelitis (EAE) model Intraperitoneal injection 8 mg/kg Once daily, starting from PID 7 until the end of the study To evaluate the effect of Sephin1 on the disease progression in EAE model mice. Results showed that Sephin1 significantly delayed disease onset, reduced oligodendrocyte and axon loss, and decreased T cell presence in the CNS. Brain. 2019 Feb 1;142(2):344-361
C57BL/6 mice G93A mtSOD1 transgenic mice Intraperitoneal injection 8 mg/kg Three times a week starting at 60 days of age Guanabenz significantly delayed disease onset, prolonged the duration of the early phase of disease, and extended survival of G93A mice. Neurobiol Dis. 2014 Nov;71:317-24

Guanabenz Acetate/氯苄氨胍醋酸盐 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) - -

Guanabenz Acetate/氯苄氨胍醋酸盐 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.

Guanabenz Acetate/氯苄氨胍醋酸盐 实验方案

计算器
存储液制备 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

Guanabenz Acetate/氯苄氨胍醋酸盐 技术信息

CAS号23256-50-0
分子式C10H12Cl2N4O2
分子量 291.13
SMILES Code ClC1=C(/C=N/NC(N)=N)C(Cl)=CC=C1.CC(O)=O
MDL No. MFCD00153801
别名 醋酸胍那苄 ;Wy8678 acetate; BR-750; Guanabenz(Acetate)
运输蓝冰
InChI Key MCSPBPXATWBACD-GAYQJXMFSA-N
Pubchem ID 5702062
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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