EGIS-8332

• CAT Number: I006629
• CAS Number: 220725-87-1
• Molecular Formula: C20H18N4O3
• Molecular Weight: 362.389
• Purity: ≥95%
• Solubility: Soluble in DMSO, not in water
• Storage: 0 - 4°C for short term or -20 °C for long term
• IUPAC Name: 7-acetyl-5-(4-aminophenyl)-8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepine-8-carbonitrile
• InChI: InChI=1S/C20H18N4O3/c1-12(25)24-20(2,10-21)9-14-7-17-18(27-11-26-17)8-16(14)19(23-24)13-3-5-15(22)6-4-13/h3-8H,9,11,22H2,1-2H3
• InChIKey: CBHCOCUJJQDHSR-UHFFFAOYSA-N
• SMILES: CC(=O)N1C(CC2=CC3=C(C=C2C(=N1)C4=CC=C(C=C4)N)OCO3)(C)C#N

EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.

Reference

1:Neuroprotective and anticonvulsant effects of EGIS-8332, a non-competitive AMPA receptor antagonist, in a range of animal models. Gigler G, Móricz K, Agoston M, Simó A, Albert M, Benedek A, Kapus G, Kertész S, Vegh M, Barkóczy J, Markó B, Szabó G, Matucz E, Gacsályi I, Lévay G, Hársing LG Jr, Szénási G.Br J Pharmacol. 2007 Sep;152(1):151-60. Epub 2007 Jul 2. PMID: 17603549 Free PMC Article2:The new 2,3-benzodiazepine derivative EGIS-8332 inhibits AMPA/kainate ion channels and cell death. Vegh MG, Kovács AD, Kovács G, Szabó G, Tihanyi K, Hársing LG Jr, Lévay G.Neurochem Int. 2007 Feb;50(3):555-63. Epub 2006 Dec 4. PMID: 17147974