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首页-小分子抑制剂&激动剂-GPCR-Vasoactive intestinal peptide receptor (VIPR)-KS-133
KS-133

Chemical Structure : KS-133

CAS No.: 2724212-01-3

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KS-133 (KS133)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    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.

    物理化学性质&存储条件

    分子量 1558.92
    分子式 C75H111N15O17S2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    Ac-CPPYLPKYLCDLI-NH2 (cyclized C1-C10, K7-D11)

    参考文献

    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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