Etazolate hydrochloride  (Synonyms: SQ 20009; EHT 0202 hydrochloride)

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 (GABA_A) 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^{[1][2][3][4][5]}.

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 (SQ 20009; 1, 3, 10 mg/kg; IP) improves recognition memory and reduces locomotor hyperactivity in a persistent manner following traumatic brain injury (TBI) in mice^[3].
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.

325.79

C₁₄H₂₀ClN₅O₂

35838-58-5

Solid

Off-white to light yellow

O=C(C1=CN=C2C(C=NN2CC)=C1N/N=C(C)\C)OCC.Cl

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* 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.

• [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]