Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 1H-Pyrazolo[3,4-b]pyridine-5-carboxylicacid, 1-ethyl-4-[2-(1-methylethylidene)hydrazinyl]-, ethyl ester, hydrochloride(1:1)
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

35838-58-5

35838-58-5 structure

Name: Etazolate hydrochloride
Chemical Name: Etazolate hydrochloride
CAS Number: 35838-58-5
Molecular Formula: C₁₄H₂₀ClN₅O₂
Molecular Weight: 325.79400
Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
Create Date: 2017-10-05 17:36:08
Modify Date: 2024-01-12 19:38:03
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[1][2][3][4][5].

Name	Etazolate hydrochloride
Synonyms	Ethyl 1-ethyl-4-(isopropylidenehydrazino)-1H-pyrazolo[3,4-b]pyridine-5-carboxylate monohydrochloride

Description	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[1][2][3][4][5].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Inflammation/Immunology Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> GABA Receptor
Target	PDE4:2 μM (IC50)
In Vitro	Etazolate hydrochloride (SQ 20009; 25 µM) 在 LtT7.TR 细胞中显着增加精氨酸酶和 ODC 蛋白质水平的表达(精氨酸酶和 ODC 分别为～3.1 倍和～1.6 倍) [2]。
In Vivo	Etazolate hydrochloride (SQ 20009; 1, 3, 10 mg/kg; 腹腔给药) 在小鼠创伤性脑损伤 (TBI) 后持续改善识别记忆并减少运动过度活跃[3]。 Etazolate hydrochloride (0.5, 1 mg/kg; 灌胃给药; 每天一次; 21 天) 在瑞士白化小鼠 (22-25 g)中显着抑制慢性不可预知的轻度应激 (CUMS) 诱导的行为 (减少蔗糖消耗并增加不动的持续时间) 和生化 (增加脂质过氧化和亚硝酸盐水平；降低谷胱甘肽、超氧化物歧化酶和过氧化氢酶活性) 的变化[4]。 Etazolate hydrochloride (0.5, 1 mg/kg; 腹腔注射; 单次) 在雄性 Wistar 大鼠 (250-275 g) 中拮抗 Reserpine (HY-N0480; 1 mg/kg;腹腔注射) 诱导的体温过低[5]< /sup>。 Animal Model: Male Swiss mice with 28-30 g[3] Dosage: 1, 3, 10 mg/kg Administration: IP 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.
References	[1]. Xuemei Wei, et al. Targeting phosphodiesterase 4 as a therapeutic strategy for cognitive improvement. Bioorg Chem. 2023 Jan;130:106278. [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. [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. [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. [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.

Density	1.25g/cm3
Boiling Point	427.6ºC at 760mmHg
Molecular Formula	C₁₄H₂₀ClN₅O₂
Molecular Weight	325.79400
Flash Point	212.4ºC
Exact Mass	325.13100
PSA	81.40000
LogP	3.31060

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H315-H319-H335
Precautionary Statements	P261-P305 + P351 + P338
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xi: Irritant;
Risk Phrases	R36/37/38
RIDADR	NONH for all modes of transport

35838-58-5	27190-69-8
1406-14-0	6138-79-0
127228-87-9	143851-98-3
929-73-7	65546-09-0
1135280-78-2	56-99-5