(E)-Guanabenz
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease.
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。
- CAS 番号: 60329-03-5
- 分子式: C8H8Cl2N4
- 分子量:231.08
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
Adrenergic Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
|
α adrenergic receptor |
Cellular Effect
|
Cell Line
|
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
|
[PMID: 28230985] |
| HEK-293T | EC50 |
0.09 μM
Compound: 16a
|
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 |
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 60329-03-5
-
分子量 231.08
-
分子式 C8H8Cl2N4
-
SMILES
ClC1=C(/C=N/NC(N)=N)C(Cl)=CC=C1
-
別名
(E)-Wy-8678
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
純度とドキュメンテーション
参考文献
[1]. Sun X, et al. Guanabenz promotes neuronal survival via enhancement of ATF4 and parkin expression in models of Parkinson disease. Exp Neurol. 2018 May;303:95-107. [Content Brief]
[2]. Xie J, et al. LC-MS/MS determination of guanabenz E/Z isomers and its application to in vitro and in vivo DMPK profiling studies. J Pharm Biomed Anal. 2021 Oct 25;205:114331. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
(E)-Guanabenz 関連分類
HY-W263279 関連分類
Powered by Bioz