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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- Purity: 98.00%
- CAS No.: 35838-58-5
- 화학식: C14H20ClN5O2
- 분자량:325.79
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보관:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Biological Activity
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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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 35838-58-5
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Appearance Solid
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분자량 325.79
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화학식 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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Synonyms
SQ 20009; EHT 0202 hydrochloride
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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 Related Classifications
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