Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. On cells, the inhibitory binding potency of palosuran against human UT receptor was lower than on membranes (IC50 = 46.2 ± 13 nM on TE 671 cells and 86 ± 30 nM on recombinant CHO cells).
Long-term treatment of streptozotocin-induced diabetic rats with palosuran improved survival, increased insulin, and slowed the increase in glycemia, glycosylated hemoglobin, and serum lipids. In mesenteric vessels, palosuran treatment up-regulated expression of RhoA and Rho-kinase, increased Rho-kinase-activity, and diminished nitric oxide (NO)/cyclic guanosine 3',5'-monophosphate (cGMP) signaling. Moreover, palosuran increased renal blood flow, sodium, and water excretion in BDL rats.
|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||DMSO: ≥ 30 mg/mL|
Palosuran treatment effective as bosentan in the treatment model of pulmonary arterial hypertension.
Pehlivan Y, et al. Inflammation. 2014 Aug;37(4):1280-8. PMID: 24604341.
Urotensin inhibition with palosuran could be a promising alternative in pulmonary arterial hypertension.
Onat AM, et al. Inflammation. 2013 Apr;36(2):405-12. PMID: 23100033.
Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects.
Sidharta PN, et al. J Clin Pharmacol. 2009 Oct;49(10):1168-75. PMID: 19625629.
JNJ-47117096 is potent and selective MELK inhibitor with IC50 of 23 nM.
Phytohemagglutinin is a lectin obtained from the red kidney bean that binds to the membranes of T-cells, stimulates metabolic activity and involves inflammatory pathways.
Apilimod is a potent IL-12/IL-23 inhibitor, and it is also a cell permeable small molecule which specifically inhibits PIKfyve with an IC50 of 14 nM in an in vitro kinase assay.
10-Hydroxy-trans-2-decenoic acid is the principal lipid component in royal jelly which is the food for queen and larvae honeybees.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.