Valerosidate 

Valerosidate is an OX2R antagonist. Valerosidate increases expression of tumor suppressor proteins p53 and PTEN, selectively reduces colon cancer cell viability, and suppresses colon cancer cell migration. Valerosidate can be used for the research of colon cancer and insomnia^[1][2].

Valerosidate (48 h) selectively inhibits cell viability in human colon cancer HCT116 cells with an IC₅₀ of 22.2 μM and a selectivity index of 3.21^[1].
Valerosidate (5.41-10.81 μM; 24 h) inhibits migration of human colon cancer cells^[1].
Valerosidate (5.41-10.81 μM; 48 h) increases the expression of tumor suppressor proteins p53 (by 26.1%) and PTEN in human colon cancer HCT116 cells^[1].
Valerosidate binds to OX2R with a favourable binding free energy of -6.01 kcal/mol, with key stabilizing interactions involving residues GLN134, PHE227, ASN324, and VAL325^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

462.49

C₂₁H₃₄O₁₁

29505-31-5

Solid

White to off-white

O[C@H]([C@H]([C@@H]([C@@H](CO)O1)O)O)[C@@H]1OCC2=CO[C@@H](OC(CC(C)C)=O)[C@@]3([H])[C@]2([H])C[C@H](O)[C@]3(O)C

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

• [1]. Yang H, et al. Discovery of a heat-generated compound DHD derived from Patrinia villosa water extract with inhibitory effects on colon cancer cells viability and migration. Front Chem. 2023 Jun 2;11:1195883.  [Content Brief]

  [2]. Shenoy AG, et al. Discovery of natural orexin 2 receptor antagonists from Valeriana species: A potential approach for insomnia treatment. Chronobiol Int. 2025;42(8):1107-1120.  [Content Brief]