Alogabat (RG7816, RO7017773)

Chemical Structure : Alogabat

CAS No.: 2230009-48-8

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货号: PC-38382Not For Human Use, Lab Use Only.

Alogabat (RG7816, RO7017773) is a potent, selective GABAA-α5 receptors positive allosteric modulator (PAM) with Ki of 7.9 nM for GABAA-α5β3γ2 receptors in rats, 37-, 26-, and 18-fold selectivity over GABAA α1β3γ2, α2β3γ2, and α3β3γ2, respectively.

规格	价格	库存
5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Alogabat (RG7816, RO7017773) is a potent, selective GABAA-α5 receptors positive allosteric modulator (PAM) with Ki of 7.9 nM for GABAA-α5β3γ2 receptors in rats, 37-, 26-, and 18-fold selectivity over GABAA α1β3γ2, α2β3γ2, and α3β3γ2, respectively.

Alogabat (RG7816, RO 7017773) has a similar pharmacological profile in human recombinant GABAA receptor subtypes.

Alogabat enhances GABA-evoked responses of rat and human α5-containing receptors by 167% and 72%, respectively.

Alogabat potentiates other receptor subtypes to a much lesser extent than α5-containing receptors.

Alogabat normalized elevated self-grooming behavior in both Cntnap2−/− and BTBR mice and exhibited antiepileptic activity in rats.

Alogabat showed beneficial effects in mouse models relevant to neurodevelopmental disorders and anti-seizure activity.

物理化学性质&存储条件

分子量	409.446
分子式	C21H23N5O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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Solubility	10 mM in DMSO
Chemical Name/SMILES	6-((5-methyl-3-(6-methylpyridin-3-yl)isoxazol-4-yl)methoxy)-N-(tetrahydro-2H-pyran-4-yl)pyridazine-3-carboxamide

参考文献

1. Patent WO2018104419A1.
2. Cecere G, et al. Front Pharmacol. 2025 Jul 21;16:1626078.