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.
別名:
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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この商品について
実験式（ヒル表記法）:
C28H22FN5O2 · xHCl
CAS番号:
分子量:
479.50 (free base basis)
UNSPSC Code:
12352211
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light
Quality Segment
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
SMILES string
Fc1c(ccc(c1)C(=O)c4c5c([n](c4)C(=O)N(C)C)cccc5C#C)C[n]2c3c(nc2C)cncc3.[Cl-].[H+]
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
Preparation Note
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.
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
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable