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Palosuran

Cat. No. M9102

All AbMole products are for research use only, cannot be used for human consumption.

Palosuran Structure
Synonym:

ACT-058362

Size Price Availability Quantity
2mg USD 210  USD210 In stock
5mg USD 275  USD275 In stock
10mg USD 430  USD430 In stock
25mg USD 770  USD770 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 418.53
Formula C25H30N4O2
CAS Number 540769-28-6
Solubility (25°C) DMSO: ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Pehlivan Y, et al. Inflammation. Palosuran treatment effective as bosentan in the treatment model of pulmonary arterial hypertension.

[2] Onat AM, et al. Inflammation. Urotensin inhibition with palosuran could be a promising alternative in pulmonary arterial hypertension.

[3] Sidharta PN, et al. J Clin Pharmacol. Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects.

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Keywords: Palosuran, ACT-058362 supplier, inhibitors, activators

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