511071

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.

• Sinônimo(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
• Fórmula empírica (Notação de Hill): C₂₈H₂₂FN₅O₂ · xHCl
• Número CAS: 189689-94-9
• Peso molecular: 479.50 (free base basis)
• Número MDL: MFCD00945301
• Código UNSPSC: 12352211
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥98% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic); protect from light
• cor: off-white
• solubilidade: water: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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
• chave InChI: AWRGBOKANQBIBM-UHFFFAOYSA-N

Descrição

Descrição geral

An orally available ethynylindole compound that potently inhibits PAF (platelet-activating factor) binding to its receptor in a competitive manner in equilibrium binding studies (K_i = 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.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable