RO 4938581

RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively) ; RO 4938581 is used in the research of cognitive dysfunction.

Product Specifications

CAS Number

[883093-10-5]

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/RO_4938581.html

Purity

99.78

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

FC(C1=C2N(C3=CC=C(Br)C=C3C4=NC=NN4C2)C=N1)F

Molecular Formula

C13H8BrF2N5

Molecular Weight

352.14

Precautions

H315, H319, H320

References & Citations

[1]Knust H, et al. The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction. Bioorg Med Chem Lett. 2009 Oct 15;19 (20) :5940-4.