Ipragliflozin significantly suppressed body weight gain at 3mg/kg. In the pioglitazone-treated group, a statistically significant increase in body weight was observed compared to CDAA diet-fed vehicle-treated rats.
|Animal models||Male Wistar rats|
|Dosages||0.3 and 3 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Ipragliflozin, an SGLT2 inhibitor, exhibits a prophylactic effect on hepatic steatosis and fibrosis induced by choline-deficient l-amino acid-defined diet in rats.
Hayashizaki-Someya Y, et al. Eur J Pharmacol. 2015 May 5;754:19-24. PMID: 25701721.
SGLT2 selective inhibitor ipragliflozin reduces body fat mass by increasing fatty acid oxidation in high-fat diet-induced obese rats.
Yokono M, et al. Eur J Pharmacol. 2014 Mar 15;727:66-74. PMID: 24486393.
NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.
Budesonide is a GC steroid commonly used for the treatment of asthma and non-infectious rhinitis.
Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
Laropiprant is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM, and exhibits > 1,000 fold selectivity over DP2 receptor (Ki=0.75 μM).
Thiazolidinediones (TZDs) are peroxisome proliferator-activated receptor γ agonists that improve insulin-mediated glucose uptake and possess beneficial vasculoprotective actions.
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