A-867744
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MedKoo CAT#: 526703

CAS#: 1000279-69-5

Description: A-867744 is a type II PAM with good potency and selectivity. A-867744 showed acceptable pharmacokinetic profile across species and brain levels sufficient to modulate alpha7 nAChRs. In a rodent model of sensory gating, A-867744 normalized gating deficits.A-867744 represents a novel class of molecules capable of allosteric modulation of the alpha7 nAChRs. A-867744 potentiated acetylcholine (ACh)-evoked currents, with an EC(50) value of approximately 1 microM.


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A-867744, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 526703
Name: A-867744
CAS#: 1000279-69-5
Chemical Formula: C20H19ClN2O3S
Exact Mass: 402.0805
Molecular Weight: 402.893
Elemental Analysis: C, 59.62; H, 4.75; Cl, 8.80; N, 6.95; O, 11.91; S, 7.96


Synonym: A-867744; A 867744; A867744.

IUPAC/Chemical Name: 4-(5-(4-Chlorophenyl)-2-methyl-3-propionylpyrrol-1-yl)benzenesulfonamide

InChi Key: ABACVOXFUHDKNZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H19ClN2O3S/c1-3-20(24)18-12-19(14-4-6-15(21)7-5-14)23(13(18)2)16-8-10-17(11-9-16)27(22,25)26/h4-12H,3H2,1-2H3,(H2,22,25,26)

SMILES Code: O=S(C1=CC=C(N2C(C)=C(C(CC)=O)C=C2C3=CC=C(Cl)C=C3)C=C1)(N)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
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 Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


References

1: Ween H, Thorin-Hagene K, Andersen E, Grønlien JH, Lee CH, Gopalakrishnan M,
Malysz J. Alpha3* and alpha 7 nAChR-mediated Ca2+ transient generation in IMR-32
neuroblastoma cells. Neurochem Int. 2010 Oct;57(3):269-77. doi:
10.1016/j.neuint.2010.06.005. Epub 2010 Jun 15. PubMed PMID: 20558224.

2: Malysz J, Anderson DJ, Grønlien JH, Ji J, Bunnelle WH, Håkerud M,
Thorin-Hagene K, Ween H, Helfrich R, Hu M, Gubbins E, Gopalakrishnan S,
Puttfarcken PS, Briggs CA, Li J, Meyer MD, Dyhring T, Ahring PK, Nielsen EØ,
Peters D, Timmermann DB, Gopalakrishnan M. In vitro pharmacological
characterization of a novel selective alpha7 neuronal nicotinic acetylcholine
receptor agonist ABT-107. J Pharmacol Exp Ther. 2010 Sep 1;334(3):863-74. doi:
10.1124/jpet.110.167072. Epub 2010 May 26. PubMed PMID: 20504915.

3: Hu M, Gopalakrishnan M, Li J. Positive allosteric modulation of alpha7
neuronal nicotinic acetylcholine receptors: lack of cytotoxicity in PC12 cells
and rat primary cortical neurons. Br J Pharmacol. 2009 Dec;158(8):1857-64. PubMed
PMID: 20050184; PubMed Central PMCID: PMC2807647.

4: Faghih R, Gopalakrishnan SM, Gronlien JH, Malysz J, Briggs CA, Wetterstrand C,
Ween H, Curtis MP, Sarris KA, Gfesser GA, El-Kouhen R, Robb HM, Radek RJ, Marsh
KC, Bunnelle WH, Gopalakrishnan M. 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. J Med Chem. 2009 May 28;52(10):3377-84. doi:
10.1021/jm9003818. PubMed PMID: 19419141.

5: Malysz J, Grønlien JH, Anderson DJ, Håkerud M, Thorin-Hagene K, Ween H,
Wetterstrand C, Briggs CA, Faghih R, Bunnelle WH, Gopalakrishnan M. 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. J Pharmacol Exp Ther. 2009
Jul;330(1):257-67. doi: 10.1124/jpet.109.151886. Epub 2009 Apr 23. PubMed PMID:
19389923.