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Chemical Structure| 540769-28-6 Chemical Structure| 540769-28-6

Structure of Palosuran
CAS No.: 540769-28-6

Chemical Structure| 540769-28-6

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Palosuran is a potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

Synonyms: ACT-058362

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Product Details of Palosuran

CAS No. :540769-28-6
Formula : C25H30N4O2
M.W : 418.53
SMILES Code : O=C(NC1=CC(C)=NC2=C1C=CC=C2)NCCN3CCC(O)(CC3)CC4=CC=CC=C4
Synonyms :
ACT-058362
MDL No. :MFCD07772352

Safety of Palosuran

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H320-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Palosuran

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CHO cells 0.1 nM–10 µM 10 minutes Evaluate Palosuran's inhibition of hU-II-induced [Ca2+]i mobilization. Results showed an IC50 of 323±67 nM, representing a 65-fold reduction in activity compared to membrane binding affinity (Ki 5 nM). Br J Pharmacol. 2008 Oct;155(3):374-86
U2OS cells 1 pM–1 µM Overnight Evaluate Palosuran's binding affinity to UT receptors in U2OS cells. Results showed a significant 54-fold loss in affinity in intact cells (Ki 276±67 nM) compared to membrane binding (Ki 5±1 nM). Br J Pharmacol. 2008 Oct;155(3):374-86
HEK293 cells 1 pM–1 µM Overnight Evaluate Palosuran's binding affinity to primate UT receptors in recombinant cell membranes. Results showed high affinity in monkey and human UT membranes (Ki values 4±1 nM and 5±1 nM, respectively), but low affinity at other mammalian UT isoforms (rodent and feline Ki >1 μM). Br J Pharmacol. 2008 Oct;155(3):374-86

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Isolated aortic rings Ex vivo organ bath 10 μM Single dose, 30 min pretreatment Evaluate Palosuran's inhibition of hU-II-induced contraction in rat isolated aortae. Results showed no significant inhibitory activity (Kb >10 μM), consistent with its low affinity at rodent UT membranes. Br J Pharmacol. 2008 Oct;155(3):374-86
Nude mice (nu/nu) U87 glioblastoma xenograft model Intratumoral injection 29 ng/kg Once daily for 15 days Test the effect of palosuran on glioblastoma growth, significantly delayed tumor growth Front Cell Dev Biol. 2021 Apr 14;9:652544

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.95mL

2.39mL

1.19mL

23.89mL

4.78mL

2.39mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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