Afizagabar

小分子

阿菲扎加巴尔

AT33292 | s44819 | S-44819 | 1398496-82-6 | GLXC-25527 | SCHEMBL12095327 | starbld0002583 | Afizagabar | 5-(4-Fluoro-1-benzothiophen-2-yl)-8-methyl-1,9-dihydro- 2H-(1,3)oxazolo(4,5-H)(2,3)benzodiazepin-2-one | 5-(4-Fluorobenzo[b]thiophen-2-yl)-8-methyl-1,

Afizagabar

A650714-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR , with an IC 50 of 585 nM for α5β2γ2 and a K i of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy. In Vitro Afizagabar (S44819) is a competitive α5-GABAAR antagonist (K b =221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague Dawley (SPRD) rats (In the eight-arm radial maze) Dosage: 1 and 3 mg/kg Administration: I.p. Result: Significantly diminished the marked increase in total errors induced by Scopolamine. Form:Solid

Afizagabar (S44819) 是α5-GABAAR GABA 结合位点上的第一类竞争性和选择性拮抗剂，对 α5β2γ2 的 IC 50 为 585 nM，对 α5β3γ2 的 K i 为 66 nM。阿非扎巴能增强海马突触的可塑性，其 p

1398496-82-6

C19H12FN3O2S

365.38 g/mol

136209703

CC1=NN=C(C2=CC3=C(C=C2C1)NC(=O)O3)C4=CC5=C(C=CC=C5S4)F

5-(4-fluoro-1-benzothiophen-2-yl)-8-methyl-1,9-dihydro-[1,3]oxazolo[4,5-h][2,3]benzodiazepin-2-one

1S/C19H12FN3O2S/c1-9-5-10-6-14-15(25-19(24)21-14)7-11(10)18(23-22-9)17-8-12-13(20)3-2-4-16(12)26-17/h2-4,6-8H,5H2,1H3,(H,21,24)

WNUWGRVHGICCLS-UHFFFAOYSA-N

CC1=NN=C(C2=CC3=C(C=C2C1)NC(=O)O3)C4=CC5=C(C=CC=C5S4)F

136209703

1398496-82-6

S44819

DMSO : 6.25 mg/mL (17.11 mM; Need ultrasonic)

1

6

1

365.063 Da

365.063 Da

91.300 Ų

26

0

669.000

0

1

3.900