Fig. 1 · Structure
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KS-133
VIPR2 Antagonist
KS-133 is a bicyclic peptide that acts as a selective antagonist of the vasoactive intestinal peptide receptor 2 (VIPR2). This compound effectively inhibits VIPR2-mediated signaling pathways, including Gq/Ca, Gs/cAMP, cAMP/PKA/ERK, and PI3K/AKT/GSK3β, and significantly reduces agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 demonstrates efficacy in modulating macrophage polarization towards the M1 phenotype and exhibits antitumor effects in colorectal cancer models by inhibiting cancer cell proliferation and altering cell cycle distribution. Additionally, KS-133 shows potential in reversing cognitive decline associated with psychiatric disorders, making it a valuable tool for research in schizophrenia, colorectal cancer, and breast cancer.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Antagonist |
| CAS Number | 2724212-01-3 |
| Applications | VIPR2 Antagonist |
| Formula | C75H111N15O17S2 |
| Molecular Weight | 1558.90 |
| SMILES | O=C1[C@]2(N(C(=O)[C@@H](NC(C)=O)CSSC[C@]3(C(=O)N[C@H](C(N[C@H](C(N[C@@H]([C@H](CC)C)C(N)=O)=O)CC(C)C)=O)CC(=O)NCCCC[C@](NC(=O)[C@]4(N(C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC5=CC=C(O)C=C5)NC(=O)[C@]6(N1CCC6)[H])CCC4)[H])(C(=O)N[C@@H](CC7=CC=C(O)C=C7)C(=O)N[C@@H](CC(C)C)C(=O)N3)[H])[H])CCC2)[H] |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.