Etazolate hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Etazolate hydrochloride 是PDE-4抑制剂和选择性的GABA-A受体调节剂[3]。
PDE-4可通过cAMP依赖和非依赖性途径调控炎症介质的释放。选择性作用于PDE-4是一种治疗与炎症相关的呼吸系统疾病的新方法,如哮喘和慢性阻塞性肺疾病[1]。
GABA-A受体的药理学调节在治疗阿尔茨海默病(AD)的中枢突方面越来越受到重视,包括神经元的存活和认知[2]。
在大鼠皮层神经元细胞中,etazolate hydrochloride(0.2 μM)通过刺激α分泌酶途径,从而诱导sAPPα的产生;通过调控GABA-A受体,阻碍皮质神经元中Aβ的神经毒性[2]。
在IIA期的研究中,对159位阿尔茨海默病患者进行超过3个月的治疗,结果显示etazolate hydrochloride与AChEI(乙酰胆碱酯酶抑制剂)联用是安全的,且耐受性良好[3]。
参考文献:
[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.
2. Alzoubi KH, Mokhemer E, et al. "Beneficial effect of etazolate on depression-like behavior and, learning, and memory impairment in a model of Parkinson's disease." Behav Brain Res. 2018 Sep 17;350:109-115. PMID:29758248
3. Alzoubi KH, Al Subeh ZY, et al. "Evaluating the protective effect of etazolate on memory impairment, anxiety- and depression-like behaviors induced by post traumatic stress disorder." Brain Res Bull. 2017 Oct;135:185-192. PMID:29107895
Physical Appearance | A solid |
Storage | Store at RT |
M.Wt | 325.8 |
Cas No. | 35838-58-5 |
Formula | C14H19N5O2·HCl |
Solubility | ≥7.75 mg/mL in DMSO; ≥9.94 mg/mL in EtOH; insoluble in H2O |
Chemical Name | ethyl 1-ethyl-4-(2-(propan-2-ylidene)hydrazinyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylate hydrochloride |
SDF | Download SDF |
Canonical SMILES | O=C(C1=CN=C2N(CC)N=CC2=C1N/N=C(C)\C)OCC.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
Wistar大鼠胚胎的脑皮质细胞 |
溶解方法 |
在蒸馏水中的溶解度为50 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应时间 |
48 h,0~2 μM |
应用 |
在皮质神经元中,0~2 μM etazolate hydrochloride可剂量依赖性地增加非淀粉样sAPPα。0.2 μM etazolate hydrochloride通过调控GABA-A受体,阻碍皮质神经元中Aβ的神经毒性,这与α-分泌酶活性和sAPPα的诱导相关。Etazolate hydrochloride通过刺激α分泌酶途径,诱导sAPPα的产生,但不影响淀粉样变性途径。 |
临床实验[2]: | |
临床模型 |
阿尔茨海默病患者 |
剂量 |
40 和 80 mg,每天两次,给药3个月,口服 |
应用 |
在IIA期的研究中,对159位阿尔茨海默病患者进行3个月的治疗,结果显示etazolate hydrochloride与AChEI(乙酰胆碱酯酶抑制剂)联用是安全的且耐受性良好。大多数精神病和神经病相关的副作用发生在高剂量组(etazolate hydrochloride 80 mg,2次/天),表明具有潜在的剂量效应关系。跟placebo组相比,胃肠道和心血管相关的副作用在etazolate hydrochloride 处理组中很少发生,表明AChEI与etazolate hydrochloride之间没有潜在的不良反应。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。 |
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. |
质量控制和MSDS
- 批次: