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Etazolate hydrochloride Catalog No.GC12771

PDE-4 inhibitor and selective GABA-A receptor modulator

Size Price Stock Qty
10mM (in 1mL DMSO)
$33.00
In stock
10mg
$74.00
In stock
50mg
$303.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Neuronal cortical cells from Wistar rat embryos

Preparation method

The solubility of this compound in sterile water is 50 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

48 h, 0~2 µM

Applications

In cortical neurons, 0~2 µM etazolate hydrochloride dose-dependently increased secreted levels of non-amyloidogenic sAPPα. etazolate hydrochloride (0.2 µM) prevented the neurotoxicity of Aβ on cortical neurons via the GABA-A receptor, which was associated with α-secretase activity and sAPPα induction. Etazolate hydrochloride induced sAPPα through the stimulation of the α-secretase pathway, and didn’t affect the amyloidogenic pathway.

Clinical experiment [2]:

Clinical models

Alzheimer’s disease patients

Dosage form

40 and 80 mg bid for 3 month, oral administration

Application

Etazolate hydrochloride in combination with one AChEI ( acetycholinesterase inhibitor) was shown to be safe and generally well tolerated in this Phase IIA study in 159 Alzheimer’s Disease patients over a 3-month treatment period. Most of psychiatric and neurologic AEs (Adverse events) were observed in the high-dose (etazolate 80 mg bid) group, suggesting a potential dose-related effect. Gastrointestinal and cardiovascular related AEs were no more frequent in the etazolate groups compared to placebo, indicating the absence of a potential clinical adverse interaction between the AChEI and etazolate hydrochloride.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Marcade M, Bourdin J, Loiseau N, et al. Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing.[J]. Journal of Neurochemistry, 2008, 106(1):392-404.

[2] Vellas B; Sol O; Snyder PJ; Ousset PJ; Haddad R; Maurin M; Lemarié JC; Désiré L; Pando MP; EHT0202/002 study group. EHT0202 in Alzheimer's disease: a 3-month, randomized, placebo-controlled, double-blind study.[J]. Current Alzheimer Research, 2011, 8(2):203-12.

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Chemical Properties

Cas No. 35838-58-5 SDF
Chemical Name ethyl 1-ethyl-4-(2-(propan-2-ylidene)hydrazinyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylate hydrochloride
Canonical SMILES O=C(C1=CN=C2N(CC)N=CC2=C1N/N=C(C)\C)OCC.Cl
Formula C14H19N5O2.HCl M.Wt 325.8
Solubility ≥3.9mg/mL in H2O Storage Store at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Etazolate hydrochloride is a PDE-4 inhibitor and selective GABA-A receptor modulator [3].

PDE-4 modulates the release of inflammatory mediators through cAMP-dependent and -independent mechanisms. Selective targeting PDE-4 is a novel therapeutic approach in the treatment of inflammation-associated respiratory diseases, such as asthma and COPD (chronic obstructive pulmonary disease) [1].

In rat neuronal cortical cells, etazolate hydrochloride (0.2 μM) induced sAPPα through the stimulation of the α-secretase pathway, and exerted a neuroprotective effect against Aβ which was associated with sAPPα induction via the GABA-A receptor [2].

In 159 Alzheimer’s Disease patients, etazolate hydrochloride in combination with one AchEI (acetycholinesterase inhibitor) was shown to be safe and generally well tolerated in the Phase IIA study over a 3-month treatment period [3].

References:
[1] Dastidar S G, Rajagopal D, Ray A.  Therapeutic benefit of PDE4 inhibitors in inflammatory diseases.[J]. Current Opinion in Investigational Drugs, 2007, 8(5):364-72.
[2] Marcade M, Bourdin J, Loiseau N, et al.  Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing.[J]. Journal of Neurochemistry, 2008, 106(1):392-404.
[3] Vellas B; Sol O; Snyder PJ; Ousset PJ; Haddad R; Maurin M; Lemarié JC; Désiré L; Pando MP; EHT0202/002 study group.  EHT0202 in Alzheimer's disease: a 3-month, randomized, placebo-controlled, double-blind study.[J]. Current Alzheimer Research, 2011, 8(2):203-12.