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。
HazMat Fee + 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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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 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% | |||||||||||||||||
| Doxazosin mesylate | ✔ | 99% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 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]. |
| 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. | |
| 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 |
| 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) | - | - |
| 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 |
|
| 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 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
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