Palosuran is a potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.
Palosuran 细胞实验
Cell Line
Concentration
Treated Time
Description
References
CHO cells
0.1 nM–10 µM
10 minutes
Evaluate Palosuran's inhibition of hU-II-induced [Ca2+]i mobilization. Results showed an IC50 of 323±67 nM, representing a 65-fold reduction in activity compared to membrane binding affinity (Ki 5 nM).
Br J Pharmacol. 2008 Oct;155(3):374-86
U2OS cells
1 pM–1 µM
Overnight
Evaluate Palosuran's binding affinity to UT receptors in U2OS cells. Results showed a significant 54-fold loss in affinity in intact cells (Ki 276±67 nM) compared to membrane binding (Ki 5±1 nM).
Br J Pharmacol. 2008 Oct;155(3):374-86
HEK293 cells
1 pM–1 µM
Overnight
Evaluate Palosuran's binding affinity to primate UT receptors in recombinant cell membranes. Results showed high affinity in monkey and human UT membranes (Ki values 4±1 nM and 5±1 nM, respectively), but low affinity at other mammalian UT isoforms (rodent and feline Ki >1 μM).
Br J Pharmacol. 2008 Oct;155(3):374-86
Palosuran 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rat
Isolated aortic rings
Ex vivo organ bath
10 μM
Single dose, 30 min pretreatment
Evaluate Palosuran's inhibition of hU-II-induced contraction in rat isolated aortae. Results showed no significant inhibitory activity (Kb >10 μM), consistent with its low affinity at rodent UT membranes.
Br J Pharmacol. 2008 Oct;155(3):374-86
Nude mice (nu/nu)
U87 glioblastoma xenograft model
Intratumoral injection
29 ng/kg
Once daily for 15 days
Test the effect of palosuran on glioblastoma growth, significantly delayed tumor growth
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