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511071

Sigma-Aldrich

PAF Receptor Antagonist, ABT-491

The PAF Receptor Antagonist, ABT-491, also referenced under CAS 189689-94-9, controls the biological activity of PAF Receptor. This small molecule/inhibitor is primarily used for Membrane applications.

Synonym(s):

PAF Receptor Antagonist, ABT-491, 1-(N,N-Dimethylcarbamoyl)-4-ethynyl-3-(3-fluoro-4-((1H-2-methylimidazo[4,5-c]pyridin-1-yl)methyl)benzoyl)-indole, HCl

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About This Item

Empirical Formula (Hill Notation):
C28H22FN5O2 · xHCl
CAS Number:
Molecular Weight:
479.50 (free base basis)
MDL number:
UNSPSC Code:
12352211
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

off-white

solubility

water: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C28H22FN5O2.ClH/c1-5-18-7-6-8-25-26(18)21(16-34(25)28(36)32(3)4)27(35)19-9-10-20(22(29)13-19)15-33-17(2)31-23-14-30-12-11-24(23)33;/h1,6-14,16H,15H2,2-4H3;1H

InChI key

AWRGBOKANQBIBM-UHFFFAOYSA-N

General description

An orally available ethynylindole compound that potently inhibits PAF (platelet-activating factor) binding to its receptor in a competitive manner in equilibrium binding studies (Ki = 0.6 or 3.8 nM, respectively, using intact human platelets or isolated rabbit platelet membrane; [PAF] = 0.6 nM), while a non-competitive inhibition is observed if the membrane-bound receptors are pre-incubated with the antagonist prior to the addition of PAF, presumably due to a slower antagonist dissociation rate. Shown to effectively antagonize PAF-induced platelet and neutrophil responses at submicromolar concentrations in vitro and exhibit in vivo efficacy in alleviating PAF-mediated inflammatory and pathological processes in various animals, including guinea pigs, mice, and rats, via either i.v. or p.o.. Reported to display high specificity toward PAF receptor as evaluated in binding assays employing a wide variety of receptors and ion channels.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Curtin, M.L., et al. 1998. J. Med. Chem.41, 74.
Albert, D.H., et al. 1998. J. Pharmacol. Exp. Ther.284, 83.
Albert, D.H., et al. 1997. Eur. J. Pharmacol.325, 69.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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