| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T78356 | ||||
| Target Name | Thromboxane-A synthase | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | CGS-22652 | Drug Info | IC50 = 2 nM | ||
| ONO-1581 | Drug Info | IC50 = 3000 nM | |||
| CGS-13080 | Drug Info | IC50 = 3.2 nM | [533494] | ||
| Action against Disease Model | NV-52 | NV-52 selectively inhibits TXS in vitro in physiological relevant concentrations, causing a reduction in thromboxane B(2) of </= 40% in association with an increase in prostaglandin E(2). NV-52 is effective in suppressing colonic inflammation in a murine model of inflammatory bowel disease. | [536468] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Gene knock-down of thromboxane A synthase 1 (TBXS) with morpholinos significantly inhibited TCDD-induced mesencephalic circulation failure. Overall similar results with selective chemicals on prostaglandin signaling were obtained for pericardial edema by TCDD. These results suggest the involvement of prostanoid synthesis pathway by way of COX2-TBXS-TP in TCDD-induced local circulation failure in developing zebrafish. | [536468] | |||
| References | |||||
| Ref 536468 | Nv-52: a novel thromboxane synthase inhibitor for the treatment of inflammatory bowel disease. Expert Opin Investig Drugs. 2007 Aug;16(8):1255-66. | ||||
| Ref 533494 | J Med Chem. 1985 Feb;28(2):164-70.Imidazo[1,5-a]pyridines: a new class of thromboxane A2 synthetase inhibitors. | ||||
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