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Restrict the search for
sulfisoxazole acetyl
to a specific field?
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
BVT-2733 is an inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) that exhibits anti-diabetic, anti-inflammatory, and anti-osteoporotic properties. BVT-2733 decreases blood glucose and serum insulin levels in animal models of hyperglycemia. BVT-2733 also attenuates arthritis severity, decreases pro-inflammatory cytokine production, and suppresses synovial inflammation. In other animal models, this compound prevents 11βHSD-induced osteogenic differentiation and suppression of osteogenesis. BVT-2733 had reasonable mouse potency (IC50 = 96nM) but was only weakly active against the human isoform (IC50 = 3341 nM). This combined with moderate mouse pharmacokinetics (F = 21%) made it a suitable in vivo tool with
which to explore the potential of 11β-HSD1 as a mechanism for the treatment of type II diabetes. In KKAy mice, oral dosing twice daily (25, 50, 100 mg/kg) of BVT-2733 lowered blood
glucose levels in a dose-dependent manner.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
K-579 ((S)-1-[4-methyl-1-(2-pyrimidinyl)-4-piperidylamino]acetyl-2-pyrrolidinecarbonitrile) is potent and slower binding dipeptidyl peptidase IV inhibitor which was investigated as an antidiabetic drug. K579 suppressed the blood glucose elevation after an oral glucose tolerance test with the increment of plasma insulin and active forms of Glucagon-like peptide-1 (GLP-1). During repetitive glucose loading using Zucker fatty rats, pretreatment with K579 attenuated the glucose excursion after the second glucose loading as well as the first glucose loading without inducing hypoglycemia.
