| Bioactivity | 5-HT4 antagonist 1 is a 5-HT4 receptor antagonist with a pKi of 9.6. | ||||||||||||
| Invitro | 5-HT4 antagonist 1 (compound 6b) is a 5-HT4 receptor antagonist with a pKi of 9.6. | ||||||||||||
| In Vivo | 5-HT4 antagonist 1 (compound 6b) demonstrates good exposure and prolongs t1/2 in other species, including the mouse (t1/2 7 h), rat (t1/2 12 h) and mini-pig (t1/2 21 h). In Phase I clinical trial, it is found that 5-HT4 antagonist 1 has good oral bioavailability with a steady state plasma t1/2 of >100 h[1]. | ||||||||||||
| Name | 5-HT4 antagonist 1 | ||||||||||||
| CAS | 261766-73-8 | ||||||||||||
| Formula | C23H36N4O5S | ||||||||||||
| Molar Mass | 480.62 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Clark RD, et al. Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1697-700. |