Α5ia (α5IA)

Names

[ Name ]:
Α5ia (α5IA)

[Synonym ]:
3-(5-methylisoazol-3-yl)-6-[(1-methyl-1,2,3-triazol-4-yl)methyloxy]-1,2,4-triazolo[3,4-a]phthalazine
| inverted exclamation mark5IA
|A5IA
3-(5-methylisoxazol-3-yl)-6-[(1-methyl-1,2,3-triazol-4-yl)methyloxy]-1,2,4-triazolo[3,4-a]phthalazine

Biological Activity

[Description]:

α5IA (L-822179) is a selective α5 GABAA receptor inverse agonist with neuroprotective potential[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[In Vitro]

α5IA (100 nM, 5 days) 可以使小鼠原代海马培养物中 Aβ 1-42 诱导的细胞死亡显着减少[1]。 Cell Viability Assay[1] Cell Line: Primary mouse hippocampal culture Concentration: 0.3 nM, 3 nM, 30 nM, 100 nM Incubation Time: 24 h Result: Significantly reduced Aβ 1-42-induced cell death by 13% at a concentration of 100 nM. Significantly decreased the expression of GABAAR α5 subunit.

[In Vivo]

α5IA (5 mg/kg, i.p., once) 可持续恢复 Ts65Dn 小鼠的空间学习能力，以及长期识别的空间记忆缺陷[2]。

[References]

[1]. Chitra Vinnakota, et al. An 5 GABAA Receptor Inverse Agonist, 5IA, Attenuates Amyloid Beta-Induced Neuronal Death in Mouse Hippocampal Cultures. Int J Mol Sci. 2020 May 6;21(9):3284.

[2]. Arnaud Duchon, et al. Long-lasting correction of in vivo LTP and cognitive deficits of mice modelling Down syndrome with an α5-selective GABAA inverse agonist. Br J Pharmacol. 2020 Mar;177(5):1106-1118.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₄N₈O₂

[ Molecular Weight ]:
362.34500

[ Exact Mass ]:
362.12400

[ PSA ]:
109.05000

[ LogP ]:
1.94840

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2934999090

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%