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MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research[1]. | [IC 50]
α1A-adrenergic receptor: 0.1 nM (IC50); α1B-adrenergic receptor: 0.15 nM (IC50); α1B-adrenergic receptor: 1.40 nM (Ki); α1D-adrenergic receptor: 0.086 nM (IC50); α1D-adrenergic receptor: 0.69 nM (Ki); 5-HT2A Receptor: 0.27 nM (IC50); 5-HT2A Receptor: 0.079 nM (Ki) | [References]
[1] Peng Wang, et al. Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension. J Med Chem. 2024 Jul 5. DOI:10.1021/acs.jmedchem.4c00626 |
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