| CAS NO: | 232271-19-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Molecular Weight (MW) | 474.33 |
|---|---|
| Formula | C24H21Cl2NO5 |
| CAS No. | 232271-19-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: ≥ 41 mg/mL |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| SMILES | O=C(O)[C@H](CC1=CC=C(C2=C(OC)C=CC=C2OC)C=C1)NC(C3=C(Cl)C=CC=C3Cl)=O |
| Synonyms | TR-14035; TR14035; TR 14035 |
| In Vitro | In vitro activity: TR-14035 is a novel, dual antagonist of alpha4beta7 integrin with IC50 of 7 nM and alpha4beta1 integrin with IC50 of 87 nM. TR14035 blocked the binding of human alpha(4)beta(7) to an (125)I-MAdCAM-Ig fusion protein with IC(50) values of 2.93 and 0.75 nM, respectively. It inhibited binding of soluble ligands to alpha(4)beta(1) or alpha(4)beta(7) on cells of human or rodent origin with similar potency. Under shear flow in vitro. TR-14035 (IC(50) alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM) has completed Phase I studies in Europe. Kinase Assay: TR-14035 is a novel, dual antagonist of alpha4beta7 integrin with IC50 of 7 nM and alpha4beta1 integrin with IC50 of 87 nM. Cell Assay: |
|---|---|
| In Vivo | TR14035 blocked adhesion to HEVs [ED(50) of 0.01-0.1 mpk i.v.]. TR-14035 was taken up by rat and human hepatocytes by an apparently single saturable mechanism with K(m) of 6.7 and 2.1 microM, respectively, and taurocholate and digoxin reduced this uptake |
| Animal model | |
| Formulation & Dosage | |
| References | J Pharmacol Exp Ther. 2002 Jul;302(1):153-62; Bioorg Med Chem. 2002 Jun;10(6):2051-66. |
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