1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. 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.

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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Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

352.14

Formula

C13H8BrF2N5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (283.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8398 mL 14.1989 mL 28.3978 mL 70.9945 mL
5 mM 0.5680 mL 2.8398 mL 5.6796 mL 14.1989 mL
10 mM 0.2840 mL 1.4199 mL 2.8398 mL 7.0994 mL
15 mM 0.1893 mL 0.9466 mL 1.8932 mL 4.7330 mL
20 mM 0.1420 mL 0.7099 mL 1.4199 mL 3.5497 mL
25 mM 0.1136 mL 0.5680 mL 1.1359 mL 2.8398 mL
30 mM 0.0947 mL 0.4733 mL 0.9466 mL 2.3665 mL
40 mM 0.0710 mL 0.3550 mL 0.7099 mL 1.7749 mL
50 mM 0.0568 mL 0.2840 mL 0.5680 mL 1.4199 mL
60 mM 0.0473 mL 0.2366 mL 0.4733 mL 1.1832 mL
80 mM 0.0355 mL 0.1775 mL 0.3550 mL 0.8874 mL
100 mM 0.0284 mL 0.1420 mL 0.2840 mL 0.7099 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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