ABT-491 Hydrochloride - CAS 189689-94-9
Catalog number: 189689-94-9
Category: Inhibitor
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Molecular Formula:
C28H23ClFN5O2
Molecular Weight:
515.97
COA:
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Targets:
Platelet-activating factor receptor (PAF-R)
Description:
ABT-491 Hydrochloride is a potent, selective and orally active platelet-activating factor receptor (PAF-R) antagonist (Ki = 0.6 nM in human platelets).
Purity:
>98%
Appearance:
Colourless oil
Synonyms:
4-ethynyl-3-[3-fluoro-4-[(2-methylimidazo[4,5-c]pyridin-1-yl)methyl]benzoyl]-N,N-dimethylindole-1-carboxamide;hydrochloride; ABT 491; ABT-491
MSDS:
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Boiling Point:
534.622 ℃ at 760 mmHg
Density:
1.143 g/cm3
InChIKey:
AWRGBOKANQBIBM-UHFFFAOYSA-N
InChI:
1S/C28H22FN5O.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
Canonical SMILES:
CC1=NC2=C(N1CC3=C(C=C(C=C3)C(=O)C4=CN(C5=CC=CC(=C54)C#C)C(=O)N(C)C)F)C=CN=C2.Cl
1.Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist.
Albert DH1, Magoc TJ, Tapang P, Luo G, Morgan DW, Curtin M, Sheppard GS, Xu L, Heyman HR, Davidsen SK, Summers JB, Carter GW. Eur J Pharmacol. 1997 Apr 23;325(1):69-80.
ABT-491 (4-ethynyl-N, N-dimethyl-3-[3-fluoro-4-[(2-methyl-1H-imidazo-[4,5-c]pyridin-1-yl)methy l]benzoyl]-1H- indole-1-carboxamide hydrochloride) is a novel PAF (platelet-activating factor) receptor antagonist with a K(i) for inhibiting PAF binding to human platelets of 0.6 nM. Binding kinetics of ABT-491 to the PAF receptor is consistent with a relatively slow off-rate of the antagonist when compared to PAF. Inhibition of PAF binding is selective and is correlated with functional antagonism of PAF-mediated cellular responses (Ca2+ mobilization, priming, and degranulation). Administration of ABT-491 in vivo leads to potent inhibition of PAF-induced inflammatory responses (increased vascular permeability, hypotension, and edema) and PAF-induced lethality. Oral potency (ED50) was between 0.03 and 0.4 mg/kg in rat, mouse, and guinea-pig. When administered intravenously in these species, ABT-491 exhibited ED50 values between 0.005 and 0.016 mg/kg.
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CAS 189689-94-9 ABT-491 Hydrochloride

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