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Art. -Nr.: HY-124057

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RO5126946

RO5126946 is a selective, orally active α7 nAChR allosteric potentiator with EC₅₀ values of 0.06 μM (hα7 nAChR) and 770 nM (α7 nAChR), and it crosses the blood-brain barrier. RO5126946 enhances synaptic transmission and positively modulates GABA-ergic responses by increasing peak current, slowing current decay, and elevating the frequency of spontaneous inhibitory postsynaptic currents, without affecting the recovery of receptors from the desensitized state. RO5126946 not only enhances subthreshold nicotine effects and improves associative learning, but also does not interfere with the original pro-cognitive effects of nicotine. RO5126946 can be used to study cognitive impairments associated with diseases such as Alzheimer's disease and schizophrenia.

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CAS. Nr.: 1137233-79-4
Formel: C₁₉H₂₁ClN₂O₄S
Molecular Weight:408.90

Speicherung:

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

RO5126946 Chemical Structure

CAS. Nr.: 1137233-79-4

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

RO5126946 (0.01-3 μM) potently potentiates nicotine-evoked currents in cultured rat hippocampal neurons via an α₇ nAChR-dependent mechanism, with an EC₅₀ of 7.7 ± 2.0 × 10^-7 M and maximum potentiation of 2800% ± 730%, and this effect is independent of glutamate or GABAₐ receptor activity^[1].
RO5126946 (0.3-1 μM) does not reactivate fully desensitized α₇ nAChRs in cultured rat hippocampal neurons^[1].
RO5126946 (0.3 μM; ~5 min) potentiates nicotine-induced increases in spontaneous inhibitory postsynaptic current frequency in cultured rat hippocampal neurons, an effect dependent on action potential propagation^[1].

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

Cell Viability Assay^[1]

Cell Line:

rat hippocampal neurons
Concentration:

0.3-1 μM
Incubation Time:

/
Result:

Couldn't reactivate fully desensitized α7 nAChRs in cultured rat hippocampal neurons.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC	Bioavailability
Rat^[1]	3 mg/kg	i.v.	3490 ± 1414 ng/mL	/	4.90 h	11,600 ng·h/mL	/
Rat^[1]	1 mg/kg	p.o.	214 ± 81 ng/mL	2.5 h	5.19 h	2280 ng·h/mL	~100 %
Rat^[1]	3 mg/kg	p.o.	1050 ± 31 ng/mL	4.67 h	4.00 h	11,800 ng·h/mL	~100 %
Rat^[1]	10 mg/kg	p.o.	3470 ± 357 ng/mL	3.33 h	2.61 h	25,900 ng·h/mL	~100 %

In Vivo

RO5126946 (3-30 mg/kg; p.o.; single dose 60 minutes before training) reverses scopolamine-induced associative memory deficits in rats, with 10 and 30 mg/kg fully restoring freezing behavior to vehicle levels^[1].
RO5126946 (1 mg/kg; p.o.; single dose 60 minutes before training) potentiates the procognitive effects of a subthreshold dose of nicotine to reverse scopolamine-induced associative memory deficits in rats^[1].
RO5126946 (3 mg/kg; p.o.; single dose 60 minutes before training) reverses scopolamine-induced associative memory deficits in rats and does not interfere with the procognitive effects of an effective dose of nicotine^[1].

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

Animal Model:

Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)^[1]
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose 60 minutes before training
Result:

Significantly reversed scopolamine-induced deficits in freezing behavior.
Resulted in a freezing percentage significantly different from both vehicle and scopolamine groups at 3 mg/kg.
Restored freezing to levels statistically indistinguishable from vehicle-treated rats at 10 and 30 mg/kg.
Showed mean pre-tone freezing <4% across all groups.

Animal Model:

Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)^[1]
Dosage:

1 mg/kg
Administration:

p.o.; single dose 60 minutes before training
Result:

Did not reverse scopolamine-induced memory deficits when administered alone.
Produced a significant reversal of scopolamine-induced memory deficits when coadministered with a subthreshold dose of nicotine.
Showed mean pre-tone freezing <2% across all groups.

Animal Model:

Sprague-Dawley (male, scopolamine-induced fear conditioning memory deficit)^[1]
Dosage:

3 mg/kg
Administration:

p.o.; single dose 60 minutes before training
Result:

Significantly reversed scopolamine-induced memory deficits when administered alone.
Maintained procognitive effect when coadministered with an effective dose of nicotine.
Showed mean pre-tone freezing <3% across all groups.

Chemical Information

CAS. Nr. 1137233-79-4
Molecular Weight 408.90
Formel C₁₉H₂₁ClN₂O₄S
SMILES

N(C(=O)C1=C(OC)C=CC(Cl)=C1)[C@H]2[C@@H](C2(C)C)C3=CC=C(S(N)(=O)=O)C=C3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Sahdeo S, et al. Characterization of RO5126946, a Novel α7 nicotinic acetylcholine receptor-positive allosteric modulator. J Pharmacol Exp Ther. 2014;350(2):455-468. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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