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.
S107 is a Type 1 ryanodine receptor (RyR1) stabilizer.
3,3’,5,5’-Tetramethylbenzidine(TMB) is a chromogenic substrate used in staining procedures in immunohistochemistry as well as being a visualising reagent used in enzyme-linked immunosorbent assays (ELISA).
Coelenterazine is the luciferin, the light-emitting molecule, used for monitoring reporter genes in BRET, ELISA and HTS techniques.
Fluorescein is a synthetic organic compound and dye.
SBI-0640756 is a first-in-class inhibitor that targets eIF4G1 and disrupts the eIF4F complex.
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