Palosuran (ACT058362)

This product is for research use only, not for human use. We do not sell to patients.

Palosuran (ACT058362)
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Size Price Stock
250mg$1550Check With Us
500mg$2350Check With Us
1g$3525Check With Us

Cat #: V20688 CAS #: 540769-28-6 Purity ≥ 99%

Description: Palosuran (ACT-058362) is a potent and orally bioavailable Urotensin-II receptor antagonist (IC50=3.6 nM)with potential use in pulmonary arterial hypertension.

References: Clozel M, et al. Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin S

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Molecular Weight (MW)418.53
Molecular FormulaC25H30N4O2
CAS No.540769-28-6
ProtocolIn VitroPalosuran (8 h) inhibits 125I-U-II binding to human UT receptor, with IC50s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells
In VivoACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure
Animal modelMale Wistar rats with renal ischemia and reperfusion
DosagesMale Wistar rats with renal ischemia and reperfusion
AdministrationI.v. (continuous infusion) for 135 min
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.3893 mL11.9466 mL23.8931 mL47.7863 mL
5mM0.4779 mL2.3893 mL4.7786 mL9.5573 mL
10mM0.2389 mL1.1947 mL2.3893 mL4.7786 mL
20mM0.1195 mL0.5973 mL1.1947 mL2.3893 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.