MK-0354 497 Oral bioavailability in preclinical species

Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue

Smiles: CC1=CN=C(C=N1)NC(=O)NC1=CC(Br)=C(C)C=C1OC[C@@H]1CNCCO1

Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer

Bezerra-Silva PC

In coculture systems of human allogeneic lymphocytes with dendritic cells (DCs) or tumor cells

MK-0354 497 Oral bioavailability in preclinical speciesMK 0354 is a partial agonist of GPR109a receptor, for hGPR109a mGPR109a with EC50 of 1. 65 1. 08 M, showed no activation of GPR109b. IC50 value: 1. 65 M (EC50, for hGPR109a), 1. 08 M (EC50, for mGPR109a) Target: GPR109ain vitro: MK 0354 demonstrated clear and statistically significant partial agonism in the cAMP assays for both the mouse and human receptors with efficacy approximately 60 70% of that of either nicotinic acid or hydroxy butyrate, a