Cligosiban (PF-3274167), a non-peptide oxytocin receptor antagonist with high oral bioavailability and good brain penetration, exhibits high affinity (Ki=9.5 nM) and excellent selectivity against vasopressin receptors, particularly V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents[1][2].
Cligosiban 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rat bladder tissue
1 µM and 10 µM
Cligosiban significantly reduced the frequency of spontaneous contractions in both young and older rat bladders
Biomedicines. 2024 Mar 18;12(3):674
NCI-H2373
45 μM
5 days
To evaluate the antiproliferative effect of Cligosiban on MM cell lines with high OXTR expression. Results showed that Cligosiban significantly inhibited the proliferation of NCI-H2373 cells.
Cancer Sci. 2021 Sep;112(9):3520-3532
Y-MESO-27
25 μM
5 days
To evaluate the antiproliferative effect of Cligosiban on MM cell lines with high OXTR expression. Results showed that Cligosiban significantly inhibited the proliferation of Y-MESO-27 cells.
Cancer Sci. 2021 Sep;112(9):3520-3532
NCI-H2052
15 μM
5 days
To evaluate the antiproliferative effect of Cligosiban on MM cell lines with high OXTR expression. Results showed that Cligosiban significantly inhibited the proliferation of NCI-H2052 cells.
Cancer Sci. 2021 Sep;112(9):3520-3532
Cligosiban 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
BALB/c nude mice
NCI-H2052 xenograft model
Oral
60 mg/kg
Every other day for a total of 10 doses
To evaluate the antitumor effect of oral Cligosiban on the NCI-H2052 xenograft model. Results showed that Cligosiban significantly inhibited tumor growth.
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