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Palosuran

Cat. No. M9102
Palosuran Structure
Synonym:

ACT-058362

Size Price Availability Quantity
2mg USD 210 In stock
5mg USD 275 In stock
10mg USD 430 In stock
25mg USD 770 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 418.53
Formula C25H30N4O2
CAS Number 540769-28-6
Purity >98%
Solubility DMSO: ≥ 30 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Palosuran, ACT-058362 supplier, inhibitors

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