Etazolate hydrochloride
Based on 1 Customer Validation
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
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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: 98.00%
- CAS 番号: 35838-58-5
- 分子式: C14H20ClN5O2
- 分子量:325.79
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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PDE4 2 μM (IC50) |
Etazolate hydrochloride (SQ 20009; 25 µM) significantly increases the expression of arginase and ODC at the protein level (∼3.1- and ∼1.6-fold for arginase and ODC, respectively) in LtT7.TR cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Etazolate hydrochloride (0.5, 1 mg/kg; p.o.; once a day during 21 days) significantly inhibits the chronic unpredictable mild stress (CUMS)-induced behavioral (decreases sucrose consumption and increases duration of immobility) and biochemical (increases lipid peroxidation and nitrite level; decreases glutathione, superoxide dismutase and catalase activity) changes in Swiss Albino mice (22-25 g)[4].
Etazolate hydrochloride (0.5, 1 mg/kg; i.p.; single dose) antagonizes the Reserpine (HY-N0480; 1 mg/kg; i.p.)-induced hypothermia in male Wistar rats (250-275 g)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss mice with 28-30 g[3]
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Dosage:1, 3, 10 mg/kg
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Administration:IP
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Result:Reduced cerebral œdema when delivered 5 min and 2 h post-TBI.
Improved recognition memory and reduces locomotor hyperactivity in a persistent manner following TBI.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 35838-58-5
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性状 Solid
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分子量 325.79
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分子式 C14H20ClN5O2
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Color Off-white to light yellow
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SMILES
O=C(C1=CN=C2C(C=NN2CC)=C1N/N=C(C)\C)OCC.Cl
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別名
SQ 20009; EHT 0202 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 66.67 mg/mL (204.64 mM; Need ultrasonic; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 (277 KB)
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SDS (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Xuemei Wei, et al. Targeting phosphodiesterase 4 as a therapeutic strategy for cognitive improvement. Bioorg Chem. 2023 Jan;130:106278. [Content Brief]
[2]. Arijit Bhattacharya, et al.Role of a differentially expressed cAMP phosphodiesterase in regulating the induction of resistance against oxidative damage in Leishmania donovani. Free Radic Biol Med. 2009 Nov 15;47(10):1494-506. [Content Brief]
[3]. Eleni Siopi, et al. Etazolate, an α-secretase activator, reduces neuroinflammation and offers persistent neuroprotection following traumatic brain injury in mice. Neuropharmacology. 2013 Apr;67:183-92. [Content Brief]
[4]. Ankur Jindal, et al. Etazolate, a phosphodiesterase 4 inhibitor reverses chronic unpredictable mild stress-induced depression-like behavior and brain oxidative damage. Pharmacol Biochem Behav. 2013 Apr;105:63-70. [Content Brief]
[5]. Ankur Jindal, et al. Antidepressant-like effect of etazolate, a cyclic nucleotide phosphodiesterase 4 inhibitor--an approach using rodent behavioral antidepressant tests battery. Eur J Pharmacol. 2012 Aug 15;689(1-3):125-31. [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 (sealed storage, away from moisture). 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 | 3.0695 mL | 15.3473 mL | 30.6946 mL | 76.7365 mL |
| 5 mM | 0.6139 mL | 3.0695 mL | 6.1389 mL | 15.3473 mL | |
| 10 mM | 0.3069 mL | 1.5347 mL | 3.0695 mL | 7.6737 mL | |
| 15 mM | 0.2046 mL | 1.0232 mL | 2.0463 mL | 5.1158 mL | |
| 20 mM | 0.1535 mL | 0.7674 mL | 1.5347 mL | 3.8368 mL | |
| 25 mM | 0.1228 mL | 0.6139 mL | 1.2278 mL | 3.0695 mL | |
| 30 mM | 0.1023 mL | 0.5116 mL | 1.0232 mL | 2.5579 mL | |
| 40 mM | 0.0767 mL | 0.3837 mL | 0.7674 mL | 1.9184 mL | |
| 50 mM | 0.0614 mL | 0.3069 mL | 0.6139 mL | 1.5347 mL | |
| 60 mM | 0.0512 mL | 0.2558 mL | 0.5116 mL | 1.2789 mL | |
| 80 mM | 0.0384 mL | 0.1918 mL | 0.3837 mL | 0.9592 mL | |
| 100 mM | 0.0307 mL | 0.1535 mL | 0.3069 mL | 0.7674 mL |
Etazolate hydrochloride 関連分類
HY-100936 関連分類
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