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Atraric acid

SKU: orb1218006

Description

Atraric acid derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases. It inhibits PTP1B activity in a dose-dependent manner with IC50 values of 51.5 uM, suggest that atraric acid has potential to treat diabetes.

Images & Validation

Key Properties

CAS Number4707-47-5
MW196.2
Purity>98% (HPLC)
FormulaC10H12O4
SMILESCC1=CC(=C(C(=C1C(=O)OC)O)C)O
TargetAndrogen Receptor (AR)
SolubilityDMSO:10 mM

Bioactivity

In Vivo
Atraric acid (10, 30 mg/kg; i.p.; single dosage) inhibits the production of pro-inflammatory cytokines and reduces pathological damages in LPS-induced endotoxin shock mice. Animal model: Female BALB/c mice (7 weeks old, 17-20 g; LPS-induced endotoxin shock). Dosage: 10, 30 mg/kg. Administration: i.p.; single dosage. Result: Inhibited the production of pro-inflammatory cytokines. Reduced pathological damages such as vasodilation and bleeding.
In Vitro
Atraric acid (10 μM; CV1 cells) represses the transactivation function mediated by Dihydrotestosterone-induced human AR. Atraric acid (10 μM; PCa cells) inhibits the expression of the PSA gene in both androgen-dependent and androgen-independent PCa cells. Atraric acid (1-300 μM; 24 h) dose-dependently inhibits pro-inflammatory cytokine, nitric oxide, prostaglandin E2 in LPS-stimulated RAW264.7 cells, but does not influence the cell viability. Atraric acid (100 and 300 μM; 18 h or 4 h) downregulates the expression of phosphorylated IκB, extracellular signal-regulated kinases (ERK) and nuclear factor kappa B (NFκB) signaling pathway to exhibit anti-inflammatory effects in LPS-stimulated RAW264.7 cells. Cell Viability Assay Cell line: RAW264.7 cells Concentration: 1-300 μM. Incubation time: 24 h. Result: Did not influence the cell viability. Western blot analysis. Cell line: RAW264.7 cells Concentration: 100 and 300 μM. Incubation time: 18 h or 4 h. Result: Inhibited LPS-Induced expression of iNOS and COX-2 in a dose-dependent manner. Suppressed LPS-stimulated phosphorylation of the Nfκb signaling pathway.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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    C10H12O4

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Protocol Information