PD 176252

Name	(S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE
Synonyms	PD 176252 (2S)-3-(1H-INDOL-3-YL)-N-[[1-(5-METHOXYPYRIDIN-2-YL)CYCLOHEXYL]METHYL]-2-METHYL-2-[(4-NITROPHENYL)CARBAMOYLAMINO]PROPANAMIDE (S)-N-[[1-(5-METHOXY-2-PYRIDINYL)CYCLOHEXYL]METHYL]-A-METHYL-A-[[-(4-NITROPHENYL)AMINO]CARBONYL]AMINO-1H-INDOLE-3-PROPANAMIDE (S)-N-[[1-(5-Methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[-(4-nitrophenyl)amino]carbonyl]amino-1H-indole-3-propanamide 1H-Indole-3-propanamide, N-[[1-(5-methoxy-2-pyridinyl)cyclohexyl]methyl]-α-methyl-α-[[[(4-nitrophenyl)amino]carbonyl]amino]-, (αS)-
CAS	204067-01-6

Molecular Formula	C32H36N6O5
Molar Mass	584.67
Density	1.297±0.06 g/cm3(Predicted)
Boling Point	838.8±65.0 °C(Predicted)
pKa	11.60±0.46(Predicted)
Storage Condition	Store at +4°C
In vitro study	PD176252 is a potent antagonist of neuromedin-B preferring (BB 1 ) and gastrin-releasing peptide-preferring (BB 2 ) receptor with K i s of 0.17 nM and 1 nM for human BB 1 and BB 2 receptors, and 0.66 nM, 16 nM for Rat BB 1 and BB 2 receptors, respectively. PD176252 inhibits acidification responses to neuromedin-B or neuromedin-C at the human BB 1 or BB 2 receptors expressed in CHO cells, with the appK B s of 4.0 nM or 13 nM, and blocks bombesin-evoked increases in intracellular calcium levels in CHO cells stably expressing human BB 1 or BB 2 receptors, with appK B s of 2.3 nM and 36 nM, respectively. PD176252 is also an agonist of N-Formyl peptide receptor1/2 (FPR1/FPR2), with EC 50 s of 0.31 and 0.66 μM in HL-60 cells. PD176252 activates Ca 2+ mobilization in HL-60 cells transfected with human FPRs (EC 50 , 0.72 ± 0.21 μM). PD176252 inhibits little specific 125 I-gastrin releasing peptide binding to NCI-H345 cells at 1 nM and suppresses almost all specific bindings at 1000 nM, with an IC 50 of 30 nM. PD176252 (10, 30 μM) significantly inhibits the growth of NCI-H345 or H1299 cells, with IC 50 s of 7 and 5 μM.
In vivo study	PD176252 (1, 10 μg, p.o.) potently inhibits the growth of the proliferation of NCI-H1299 xenografts in nude mice.

biological activity	PD176252 is a potent BB1 and BB2 antagonist, it can inhibit the activity of human BB1 and BB2 receptors and rat BB1 and BB2 receptors with Ki values of 0.17 nM,1 nM and 0.66 nM,16 nM, respectively; PD176252 is also an agonist of FPR1/FPR2, with EC50 values of 0.31 and 0.66 μm in HL-60 cells, respectively.
Target	Ki: 0.17 nM (Human BB 1 receptor), 0.66 nM (Rat BB 1 receptor), 1 nM (Human BB 2 receptor), 16 nM (Rat BB 2 receptor) EC50: 0.31 μm (FPR1), 0.66 μm (FPR2)

Last Update：2024-04-09 20:49:11