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Chemical Structure : KS-133
Catalog No.: PC-20659Not For Human Use, Lab Use Only.
KS-133 (KS133) is a potent, selective bicyclic peptide antagonist of vasoactive intestinal peptide receptor 2 (VIPR2) with IC50 of 24.8 nM in Ca influx assays.
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KS-133 (KS133) is a potent, selective bicyclic peptide antagonist of vasoactive intestinal peptide receptor 2 (VIPR2) with IC50 of 24.8 nM in Ca influx assays.
KS-133 does not antagonize VIP-VIPR1 or PACAP-PAC1 signaling pathways up to 5 μM.
KS-133 antagonized VIP-VIPR2 signaling pathway in a peptide concentration-dependent manner (IC50=500 nM) in cAMP assays, without VIPR2 agonist activity up to 5 μM.
The selective VIPR2 agonist BAY 55-9837 (20 µg/mouse) significantly increased phosphorylated CREB in the prefrontal cortex, KS-133 (20 nmol/mouse) coadministration blocked this effect.
KS-133 exhibited in vivo pharmacological efficacies in a mouse model of psychiatric disorders through early postnatal activation of VIPR2.
KS-133 dose-dependently inhibited VIP-induced cell migration in VIPR2-overexpressing MDA-MB-231 cells.
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| Appearance | Solid | |
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10 mM in DMSO |
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1. Sakamoto K, et al. Front Pharmacol (2021) 12:751587.
2. Satoshi Asano, et al. Front Oncol. 2022 Sep 27;12:852358.
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