Guanabenz
Based on 4 publication(s) in Google Scholar
Guanabenz is an orally active α-2-adrenoceptor agonist. Guanabenz has antihypertensive effect and antiparasitic activity. Guanabenz interferes ER stress-signalling and has protective effects in cardiac myocytes. Guanabenz also is used for the research of high blood pressure.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.85%
- CAS 番号: 5051-62-7
- 分子式: C8H8Cl2N4
- 分子量:231.08
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Guanabenz
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生物活性
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Toxoplasma |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
4.85 μM
Compound: Guanabenz
|
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
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[PMID: 28230985] |
| HEK-293T | EC50 |
0.09 μM
Compound: 16a
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Agonist activity at human TAAR1 receptor expressed in HEK293T cells cotransfected with beta-2 receptor assessed as cAMP production by BRET assay
Agonist activity at human TAAR1 receptor expressed in HEK293T cells cotransfected with beta-2 receptor assessed as cAMP production by BRET assay
|
10.1039/C5MD00400D |
Guanabenz (0.5-50 μM, 24 h) is treated with increasing concentrations for 24 hours not affect cell viability[1].
Guanabenz (0.5-50 μM, 24 h) alone not affects the UPR targets, neither on mRNA or protein level nor the phosphorylation status of eIF2a. Guanabenz also not induces GADD34 or the constitutively active form CReP[1].
Guanabenz (0.5-50 μM, 24 h) alone not induces ER stress in neonatal rat cardiomyocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neonatal rat cardiac myocytes (NRCM)
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Concentration:0.5–50 μM
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Incubation Time:24 h
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Result:Did not affect cell survival.
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Cell Line:Neonatal rat cardiac myocytes (NRCM)
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Concentration:0.5–50 μM
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Incubation Time:24 h
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Result:Did not affect levels of UPR targets.
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Cell Line:Neonatal rat cardiac myocytes (NRCM)
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Concentration:0.5–50 μM
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Incubation Time:24 h
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Result:Increased the levels of low panel concentration-dependent UPR targets proteins.
Guanabenz (5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks) reverses Toxoplasma-induced hyperactivity in latently infected mice[2].
Guanabenz (100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min) reduces sympathetic outflow, heart rate and blood pressure in debuffered cats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cJ mice[2]
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Dosage:5 mg/kg
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Administration:5 mg/kg/day; i.p. ; for 3 weeks
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Result:Reduced the latent brain cysts in both male and female BALB/cJ mice.
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Animal Model:BALB/cJ mice[2]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:5 mg /kg/d, i.p., oral; 10 mg/kg/d, gavage; for 3 weeks
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Result:Reversed parasite-induced hyperactivity to near-baseline levels.
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Animal Model:Cats[3]
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Dosage:100 and 320 μg/kg and 1 mg/kg
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Administration:100 and 320 μg/kg and 1 mg/kg, i.v., over a period of 5 min at intervals of 40 min
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Result:Declined markedly blood pressure and nerve activity.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 5051-62-7
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性状 Solid
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分子量 231.08
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分子式 C8H8Cl2N4
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Color White to off-white
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SMILES
ClC1=C(/C=N/NC(N)=N)C(Cl)=CC=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Nature
2023 Sep;621(7977):188-195. PMID: 37648854 -
Cancer Lett
Repurposing the Neurokinin-1 receptor antagonist Aprepitant to eradicate relapsed/refractory acute lymphoblastic leukemia via mitochondria-driven necroptosis. [Abstract]2026 May 24:218621. PMID: 42184918 -
Cell Rep
2019 Dec 3;29(10):2929-2935.e4. PMID: 31801060 -
Brain Res Bull
The neuroprotective effect of guanabenz combined with α-lipoic acid in the hSOD1-G93A amyotrophic lateral sclerosis model. [Abstract]2026 Jun 1:239:111890. PMID: 41991114
溶剤 & 溶解度
DMSO : 16.67 mg/mL (72.14 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (557 KB)
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- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Christiane Neuber, et al. Guanabenz interferes with ER stress and exerts protective effects in cardiac myocytes. PLoS One. 2014 Jun 3;9(6):e98893. [Content Brief]
[2]. Jennifer Martynowicz, et al. Guanabenz Reverses a Key Behavioral Change Caused by Latent Toxoplasmosis in Mice by Reducing Neuroinflammation. mBio. 2019 Apr 30;10(2):e00381-19. [Content Brief]
[3]. T Baum, et al. Studies on the centrally mediated hypotensive activity of guanabenz. Eur J Pharmacol. 1976 May;37(1):31-44. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3275 mL | 21.6375 mL | 43.2751 mL | 108.1876 mL |
| 5 mM | 0.8655 mL | 4.3275 mL | 8.6550 mL | 21.6375 mL | |
| 10 mM | 0.4328 mL | 2.1638 mL | 4.3275 mL | 10.8188 mL | |
| 15 mM | 0.2885 mL | 1.4425 mL | 2.8850 mL | 7.2125 mL | |
| 20 mM | 0.2164 mL | 1.0819 mL | 2.1638 mL | 5.4094 mL | |
| 25 mM | 0.1731 mL | 0.8655 mL | 1.7310 mL | 4.3275 mL | |
| 30 mM | 0.1443 mL | 0.7213 mL | 1.4425 mL | 3.6063 mL | |
| 40 mM | 0.1082 mL | 0.5409 mL | 1.0819 mL | 2.7047 mL | |
| 50 mM | 0.0866 mL | 0.4328 mL | 0.8655 mL | 2.1638 mL | |
| 60 mM | 0.0721 mL | 0.3606 mL | 0.7213 mL | 1.8031 mL |