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/ Guanfacine HCl/盐酸胍法辛

Guanfacine HCl/盐酸胍法辛 {[allProObj[0].p_purity_real_show]}

货号：A810155 同义名： 胍法辛盐酸盐 / Guanfacine (hydrochloride); Guanfacine Hydrochloride

Guanfacine HCl 是一种中枢作用型 α2-肾上腺素能受体激动剂，具有 α2-肾上腺素能受体选择性，其 Kd 值为 31 nM，并且对 α2B-肾上腺素能受体显示 60 倍的选择性，从而降低心率及外周血管阻力。

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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+
Guanfacine HCl/盐酸胍法辛 化学结构 CAS号：29110-48-3
Guanfacine HCl/盐酸胍法辛 化学结构
CAS号：29110-48-3
Guanfacine HCl/盐酸胍法辛 3D分子结构
CAS号：29110-48-3
Guanfacine HCl/盐酸胍法辛 化学结构 CAS号：29110-48-3
Guanfacine HCl/盐酸胍法辛 3D分子结构 CAS号：29110-48-3
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Guanfacine HCl/盐酸胍法辛 纯度/质量文件 产品仅供科研

货号：A810155 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
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 +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 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。

Guanfacine HCl/盐酸胍法辛 生物活性

描述 Guanfacine hydrochloride, an anti-hypertensive agent. Extended-release guanfacine appears to be safe and effective for reducing hyperactivity, impulsiveness, and distractibility in children with ASD (autism spectrum disorder)[3]. Guanfacine lowers blood pressure by activating CNS alpha adrenoreceptors, which results in sympathetic outflow leading to reduced vascular tone. Guanfacine is rapidly and completely absorbed from the gastrointestinal tract and apparently undergoes extensive distribution to all tissues. Guanfacine's adverse reactions include dry mouth, sedation, and constipation. Adverse effects and reaction to sudden withdrawal of the drug may be less severe with guanfacine than with clonidine[4]. Guanfacine extended release (ER), as a new option to the treatment of attention deficit hyperactivity disorder, which acts at postsynaptic level. Guanfacine stimulates postsynaptic alfa-2A adrenergic receptors so it inhibits the production of cAMP and closes HCN channels enhancing the effectiveness of the signal of the pyramidal neurons of the prefrontal cortex, thus improving working memory and attention[5].

Guanfacine HCl/盐酸胍法辛 细胞实验

Cell Line
Concentration Treated Time Description References
human induced neurons 5 µM 30 mins Activation of α2A adrenergic receptor, increasing synaptic vesicle numbers Cell. 2019 Oct 3;179(2):498-513. e22
Human iPSC-derived neurons 10 µM 30 minutes Evaluate the effect of Guanfacine on cofilin phosphorylation in human neurons. Results showed that Guanfacine failed to induce significant changes in cofilin phosphorylation. Mol Psychiatry. 2023 Feb;28(2):588-600
Neuro2A cells 10 µM 30 minutes Evaluate the effect of Guanfacine on cofilin phosphorylation. Results showed that Guanfacine failed to induce significant changes in cofilin phosphorylation. Mol Psychiatry. 2023 Feb;28(2):588-600
4T1 breast cancer cells 0, 0.625, 1.25, 2.5, or 5 mg/L 4 hours To evaluate the cytotoxicity of GFC by MTT assay, the results showed that GFC had no obvious cell suppression phenomenon without laser irradiation; under laser irradiation, CeG showed strong cell suppression ability. ACS Appl Mater Interfaces. 2025 Mar 19;17(11):16437-16452
4T1 breast cancer cells 4.6 mg/L 2, 6, or 12 hours To evaluate the uptake behavior of GFC in 4T1 cells, the results showed that CeG nanoparticles formed by self-assembly of GFC and Ce6 had higher cellular uptake efficiency than free Ce6. ACS Appl Mater Interfaces. 2025 Mar 19;17(11):16437-16452

Guanfacine HCl/盐酸胍法辛 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Α2AAR deficient mice Intraperitoneal injection 0.5 mg/kg Single injection Evaluate the effect of Guanfacine on fear memory reconsolidation. Results showed that Guanfacine had no significant effect on fear memory reconsolidation. Mol Psychiatry. 2023 Feb;28(2):588-600
Mice FosTRAP mice Intraperitoneal injection 1 mg/kg Single injection To study the neuronal population activated by Guanfacine in the BNST and its role in stress and anxiety-like behavior. Results showed that Guanfacine activates a specific neuronal population in the BNST via α2a-AR signaling, which plays an important role in stress and anxiety-like behavior. Neuropsychopharmacology. 2023 Jul;48(8):1133-1143
C57BL/6J mice Anxiety- and depression-like behavior models Intraperitoneal injection 0.15 mg/kg Single administration, 30 minutes before testing To investigate the effects of Guanfacine on anxiety- and depression-like behaviors through α2AR and β2 nAChRs signaling pathways in the amygdala. Results showed that Guanfacine produces anxiolytic- and antidepressant-like effects by activating α2ARs in the amygdala, and these effects depend on β2 nAChRs signaling in the amygdala. Neuropsychopharmacology. 2018 Sep;43(10):2118-2125
Mice VB6-deficient mouse model Subcutaneous injection 1.0 mg/kg/day Once daily for one week Inhibiting NA release and ameliorating behavioral deficits in VB6-deficient mice Transl Psychiatry. 2021 May 3;11(1):262

Guanfacine HCl/盐酸胍法辛 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
NCT02204410 Attention Deficit Hyperactivit... 展开 >>y Disorder Deficient Emotional Self-Regulation 收起 << Phase 4 Completed - United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 收起 <<
NCT01172288 Tourettes Syndrome ... 展开 >> Tic 收起 << Phase 2 Completed - United States, Connecticut ... 展开 >> Yale Child Study Center New Haven, Connecticut, United States, 06520 收起 <<
NCT00684489 Hypertension Not Applicable Completed - -

Guanfacine HCl/盐酸胍法辛 参考文献

[1]Gillis NK, Zhu HJ, et al. An in vitro evaluation of guanfacine as a substrate for P-glycoprotein. Neuropsychiatr Dis Treat. 2011;7:501-5.

[2]Sagvolden T. The alpha-2A adrenoceptor agonist guanfacine improves sustained attention and reduces overactivity and impulsiveness in an animal model of Attention-Deficit/Hyperactivity Disorder (ADHD). Behav Brain Funct. 2006 Dec 15;2:41.

[3]Board AW, Perry VP, Shepperson BE, Nyman CE, Carchman SH. A postmarketing evaluation of guanfacine hydrochloride in mild to moderate hypertension. Clin Ther. 1988;10(6):761-775

[4]Cornish LA. Guanfacine hydrochloride: a centrally acting antihypertensive agent. Clin Pharm. 1988;7(3):187-197

[5]Alamo C, López-Muñoz F, Sánchez-García J. Mechanism of action of guanfacine: a postsynaptic differential approach to the treatment of attention deficit hyperactivity disorder (adhd). Actas Esp Psiquiatr. 2016;44(3):107-112

Guanfacine HCl/盐酸胍法辛 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.70mL

3.54mL

1.77mL

35.39mL

7.08mL

3.54mL

Guanfacine HCl/盐酸胍法辛 技术信息

CAS号29110-48-3
分子式C9H10Cl3N3O
分子量 282.55
SMILES Code O=C(NC(N)=N)CC1=C(Cl)C=CC=C1Cl.[H]Cl
MDL No. MFCD00798230
别名 胍法辛盐酸盐 ;Guanfacine (hydrochloride); Guanfacine Hydrochloride; Intuniv; Tenex; Guanfacine
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature
溶解方案

DMSO: 30 mg/mL(106.17 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: 20 mg/mL(70.78 mM)，配合低频超声助溶

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
方案 三

Tags: Guanfacine | 29110-48-3 | α2A Agonist | GPCR/G Protein | Neuronal Signaling | Adrenergic Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Guanfacine HCl/盐酸胍法辛 纯度/质量文件 | Guanfacine HCl/盐酸胍法辛 亚型比较 | Guanfacine HCl/盐酸胍法辛 生物活性 | Guanfacine HCl/盐酸胍法辛 临床数据 | Guanfacine HCl/盐酸胍法辛 参考文献 | Guanfacine HCl/盐酸胍法辛 实验方案 | Guanfacine HCl/盐酸胍法辛 技术信息

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