Omtriptolide

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

Product information

CAS Number: 195883-06-8

Molecular Weight: 460.47

Formula: C24H28O9

Chemical Name: 4-{[(1S, 2S, 4S, 5S, 7S, 8R, 9R, 11S, 13S)-1-methyl-17-oxo-7-(propan-2-yl)-3, 6, 10, 16-tetraoxaheptacyclo[11.7.0.0, .0, .0, .0, .0, ]icos-14(18)-en-8-yl]oxy}-4-oxobutanoic acid

Smiles: C[C@]12CCC3=C(COC3=O)[C@@H]1C[C@@H]1O[C@]31[C@H](OC(=O)CCC(O)=O)[C@]1(O[C@H]1[C@@H]1O[C@]231)C(C)C

InChiKey: HROMYAWHLUOUPY-AHCCQAQQSA-N

InChi: InChI=1S/C24H28O9/c1-10(2)22-17(32-22)18-24(33-18)21(3)7-6-11-12(9-29-19(11)28)13(21)8-14-23(24,31-14)20(22)30-16(27)5-4-15(25)26/h10,13-14,17-18,20H,4-9H2,1-3H3,(H,25,26)/t13-,14-,17-,18-,20+,21-,22-,23+,24+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: H2O : 1.39 mg/mL (3.02 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. 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. 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. 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).

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.

Products are for research use only. Not for human use.