[CAS NO. 540769-28-6] Palosuran

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [540769-28-6]

Catalog

HY-10655

Brand

MCE

CAS

540769-28-6

DESCRIPTION [540769-28-6]

Overview

MDL	MFCD07772352
Molecular Weight	418.53
Molecular Formula	C25H30N4O2
SMILES	OC(CC1=CC=CC=C1)(CC2)CCN2CCNC(NC3=CC(C)=NC4=CC=CC=C34)=O

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor , with an IC ₅₀ of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats ^[1] ^[2] .

IC50 & Target

IC50: 3.6 nM (human urotensin II receptor) ^[1]

In Vitro

Palosuran (8 h) inhibits ¹²⁵ I-U-II binding to human UT receptor, with IC ₅₀ s of 46.2 nM on TE 671 cells and 86 nM on recombinant CHO cells ^[1] .
Palosuran inhibits Ca ²⁺ mobilization in response to human U-II in CHO cells expressing human and rat UT receptor with IC ₅₀ s of 17 and >10000 nM, respectively ^[1] .
Palosuran (0.12-10000 nM; 20 min) inhibits human U-II induced MAPK phosphorylation in a dose-dependent manner in recombinant CHO cells, with an IC ₅₀ of 150 nM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ACT-058362 (10 mg/kg/h; i.v.) fully prevents the decrease in renal blood flow after ischemia in rats without decreasing blood pressure ^[1] .
Palosuran (300 mg/kg/d; p.o. for 16 weeks) improves the survival, increases insulin, and slows the increase in glycemia, glycosylated hemoglobin, and serum lipids in streptozotocin-induced diabetic rats ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Wistar rats with renal ischemia and reperfusion ^[1]
Dosage:	20 mg/kg/h for 135 min
Administration:	I.v. (continuous infusion) for 135 min
Result:	Restored renal blood flow to baseline values at 30 min after reperfusion and by 60 min increased renal blood flow by 12% above baseline values. Did not significantly alter mean arterial blood pressure (MAP) and heart rate (HR).

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 119.47 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3893 mL	11.9466 mL	23.8932 mL
5 mM	0.4779 mL	2.3893 mL	4.7786 mL
10 mM	0.2389 mL	1.1947 mL	2.3893 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.67 mg/mL (3.99 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 1.67 mg/mL (3.99 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 1.67 mg/mL (3.99 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

Urea, N-[2-[4-hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N′-(2-methyl-4-quinolinyl)-

N-[2-[4-Hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N′-(2-methyl-4-quinolinyl)urea

1-[2-(4-Benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea

Palosuran

ACT 058362