Atraric acid

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

阿彻瑞克酸衍生物作为 AR 拮抗剂的新型治疗化合物的新化学先导结构。

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.

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.

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.

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Endocrinology/Hormones

Androgen Receptor (AR)

Androgen Receptor|PTP1B

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4707-47-5

196.2

C10H12O4

>98% (HPLC)

DMSO:10 mM

CC1=CC(=C(C(=C1C(=O)OC)O)C)O

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(-20℃)

With Ice Pack

≥ 2 years