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FK 888

FK 888 ??? ???
?? ??:
138449-07-7
???:
FK 888
???(??):
FK 888;FK888 hydrate;N(2)-(4-Hydroxy-1-(1-methyl-1H-indol-3-yl)carbonyl-L-prolyl)-N-methyl-N-phenylmethyl-3-(2-naphthyl)-L-alaninamide;(4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide;L-Alaninamide, (4R)-4-hydroxy-1-((1-methyl-1H-indol-3-yl)carbonyl)-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-;L-Alaninamide, trans-4-hydroxy-1-((1-methyl-1H-indol-3-yl)carbonyl)-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-;N2-[(4R)-4-hydroxyl-1-(1-methyl-1H-indol-3-yl)carbonyl-L-prolyl]-N-methyl-N-phenylmethyl-3-(2-naphthyl)-L-alaninamide hydrate;(4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide hydrate
CBNumber:
CB8785831
???:
C36H36N4O4
??? ??:
588.7
MOL ??:
138449-07-7.mol

FK 888 ??

?? ?
901.9±65.0 °C(Predicted)
??
1.26±0.1 g/cm3(Predicted)
?? ??
Store at -20°C
???
DMSO: ≥13mg/mL
??? ??
??
?? ?? (pKa)
13.01±0.40(Predicted)
??
???? ?????
optical activity
[α]/D -135 to -145°, c = 1 in methanol

??

WGK ?? 3

FK 888 C??? ??, ??, ??

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FK 888 is a neurokinin NK1 receptor antagonist, which is active both in vivo and in vitro.

???? ??

Selective, high affinity tachykinin NK 1 receptor antagonist (K i = 0.69 nM) that displays 320-fold selectivity for human over rat NK 1 receptors. Inhibits substance P-induced contraction of isolated guinea pig trachea (IC 50 = 32 nM) and inhibits substance P-induced airway constriction in vivo following i.v. and oral administration.

FK 888 ?? ?? ? ???

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FK 888 ?? ??

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