Etazolate hydrochloride
目录号 : GC12771
PDE-4 inhibitor and selective GABA-A receptor modulator
Cas No.:35838-58-5
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
Neuronal cortical cells from Wistar rat embryos |
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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]: | |
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Clinical models |
Alzheimer’s disease patients |
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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. | |
| Cas No. | 35838-58-5 | SDF | |
| 化学名 | 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 | ||
| 分子式 | C14H19N5O2.HCl | 分子量 | 325.8 |
| 溶解度 | ≥ 3.9mg/mL in Water | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0694 mL | 15.3468 mL | 30.6937 mL |
| 5 mM | 0.6139 mL | 3.0694 mL | 6.1387 mL |
| 10 mM | 0.3069 mL | 1.5347 mL | 3.0694 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet