1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. GABA Receptor

RO 4938581 

Cat. No.: HY-107489
Handling Instructions

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.

For research use only. We do not sell to patients.

RO 4938581 Chemical Structure

RO 4938581 Chemical Structure

CAS No. : 883093-10-5

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

Ki: 4.6 nM (GABAA α5β3γ2a), 174 nM (GABAA α1β3γ2a), 185 nM (GABAA α2β3γ2a), 80 nM (GABAA α3β3γ2a)[1]

In Vitro

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)[1].

In Vivo

RO 4938581 (0.3-1 mg/kg, p.o.) reverses a working memory impairment induced by scopolamine the delayed match to position (DMTP) task and a spatial learning impairment induced by diazepam (RO 4938581; 1-10 mg/kg, po)[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8398 mL 14.1989 mL 28.3978 mL
5 mM 0.5680 mL 2.8398 mL 5.6796 mL
10 mM 0.2840 mL 1.4199 mL 2.8398 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

352.14

Formula

C₁₃H₈BrF₂N₅

CAS No.

883093-10-5

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
RO 4938581
Cat. No.:
HY-107489
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RO 4938581

Cat. No.: HY-107489