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Omtriptolide

Katalog-Nr.GC33857 Copy One-Click Copy Product Info

Omtriptolid (PG490-88) ist ein abgeleitetes Prodrug von Triptolid, gereinigt aus dem chinesischen Kraut.

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Omtriptolide Chemische Struktur

Cas No.: 195883-06-8

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10mM (in 1mL DMSO)
419,00 $
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1mg
138,00 $
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5mg
414,00 $
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10mg
597,00 $
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25mg
1.195,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of Omtriptolide

Omtriptolide (PG490-88) is a water soluble derivative prodrug of triptolide purified from the Chinese herb.

Triptolide, a traditional Chinese medicine, has anti-inflammatory, antiproliferative, and proapoptotic properties[1].

In a mouse model of cisplatin-induced AKI, omtriptolide results in a significant decrease in blood urea nitrogen (BUN), serum creatinine, and acute tubular necrosis (ATN) score, and a nonsignificant increase in tubular apoptosis score in AKI. The protection of omtriptolide against AKI is associated with a decrease in p-ERK and is independent of MKP-1 and proinflammatory cytokines[1]. In a mouse heterotopic tracheal allograft model of obliterative airway disease, omtriptolide attenuates airway obliteration and inhibits accumulation of inflammatory cells, and therefore may have preventive or therapeutic benefits for patients with obliterative airway disease following lung transplantation[2]. Omtriptolide inhibits fibrosis in the bleomycin group when given the same day or 5 days after bleomycin. Omtriptolide also markedly reduces the number of myofibroblasts in the bleomycin treatment group[3]. Omtriptolide inhibits in vivo both CD4+Vbeta3+ and CD8+Vbeta3+ T cell (alloreactive T cells in this model) expansion in the spleen by 64.09 and 34.02%, respectively, at the time when Vbeta3+ cell expansion is in the logarithmic phase (day 3 after transplantation)[4].

[1]. Kim HJ, et al. The water-soluble triptolide derivative PG490-88 protects against cisplatin-induced acute kidney injury. J Pharmacol Exp Ther. 2014 Jun;349(3):518-25. [2]. Leonard CT, et al. PG490-88, a derivative of triptolide, attenuates obliterative airway disease in a mouse heterotopic tracheal allograft model. J Heart Lung Transplant. 2002 Dec;21(12):1314-8. [3]. Krishna G, et al. PG490-88, a derivative of triptolide, blocks bleomycin-induced lung fibrosis. Am J Pathol. 2001 Mar;158(3):997-1004. [4]. Chen BJ, et al. Prevention of graft-versus-host disease by a novel immunosuppressant, PG490-88, through inhibition of alloreactive T cell expansion. Transplantation. 2000 Nov 27;70(10):1442-7.

Protocol of Omtriptolide

Animal experiment:

Mice: Omtriptolide (0.25 mg/kg per day) is started immediately after the transplant and 10 control mice receive intraperitoneal injections of sterile water each day. The mice are then maintained for 28 days until killing, at which time the mice are administered CO2 inhalation, and cervical dislocation is performed. Trachea is divided for histologic staining and immunohistochemistry [2].

References:

[1]. Kim HJ, et al. The water-soluble triptolide derivative PG490-88 protects against cisplatin-induced acute kidney injury. J Pharmacol Exp Ther. 2014 Jun;349(3):518-25.
[2]. Leonard CT, et al. PG490-88, a derivative of triptolide, attenuates obliterative airway disease in a mouse heterotopic tracheal allograft model. J Heart Lung Transplant. 2002 Dec;21(12):1314-8.
[3]. Krishna G, et al. PG490-88, a derivative of triptolide, blocks bleomycin-induced lung fibrosis. Am J Pathol. 2001 Mar;158(3):997-1004.
[4]. Chen BJ, et al. Prevention of graft-versus-host disease by a novel immunosuppressant, PG490-88, through inhibition of alloreactive T cell expansion. Transplantation. 2000 Nov 27;70(10):1442-7.

Chemical Properties of Omtriptolide

Cas No. 195883-06-8 SDF
Canonical SMILES C[C@@]([C@@]1([H])C[C@@H]2O3)(CCC4=C1COC4=O)[C@]5([C@H]([C@H]6[C@]7(C(C)C)O6)O5)[C@]23[C@@H]7OC(CCC(O)=O)=O
Formula C24H28O9 M.Wt 460.47
Löslichkeit H2O : 1.39 mg/mL (3.02 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Omtriptolide

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1717 mL 10.8585 mL 21.7169 mL
5 mM 434.3 μL 2.1717 mL 4.3434 mL
10 mM 217.2 μL 1.0858 mL 2.1717 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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