BiochemProbe — Life Science Research Reagents

A-867744 free base · Synonyms: A 867744 · A867744

A-867744 is a highly potent and selective type II positive allosteric modulator of the alpha7 nicotinic acetylcholine receptors.

For research use only. Not for human or veterinary use.

Target nAChR
Research area Neurological Disease
Purity >98% Stock Inquire

A-867744 structure

CAS No.: 1000279-69-5

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
100 mg USD 400.00 BP-02381-100mg In stock Get quote
250 mg USD 600.00 BP-02381-250mg Inquire Get quote
500 mg USD 900.00 BP-02381-500mg In stock Get quote
1 g USD 1,485.00 BP-02381-1g In stock Get quote
2 g Inquire BP-02381-2g In stock Inquire
5 g Inquire BP-02381-5g In stock Inquire

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Description

A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.

Biological activity

A 867744 is a positive allosteric modulator of α7 nAChRs (IC50 values are 0.98 and 1.12 μM for human and rat α7 receptor ACh-evoked currents respectively, in X. laevis oocytes). Displays no activity at 5-HT3A, α3β4 or α4β2 nAChRs. Brain penetrant.

Identifiers

SMILES
O=S(C1=CC=C(C=C1)N2C(C)=C(C=C2C3=CC=C(C=C3)Cl)C(CC)=O)(N)=O
InChIKey
ABACVOXFUHDKNZ-UHFFFAOYSA-N

Specifications

MW (average)
402.8940
Formula
C20H19ClN2O3S
CAS No.
1000279-69-5
Physical state
Solid
Color
White to yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 3 years; 4℃, 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

In vitro
DMSO : ≥ 100 mg/mL

References

[1] Ramin Faghih, et al. Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor
[2] Joseph Newcombe, et al. Diversity of Nicotinic Acetylcholine Receptor Positive Allosteric Modulators Revealed by Mutagenesis and a Revised Structural Model
[3] John Malysz, et al. In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile
[4] John Malysz, et al. In vitro pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107
[5] Krisztina Pesti, et al. Type I-like behavior of the type II α7 nicotinic acetylcholine receptor positive allosteric modulator A-867744

Same target

Search nAChR

Same research area

Search Neurological Disease