Palosuran hydrochloride - 10mM in DMSO , CAS No.2469274-58-4

CAS: 2469274-58-4 Cat. No.: P656643 Formula: C₂₅H₃₁ClN₄O₂ Peso molecolare: 454.99 PubChem CID: 137891318

QUALITÀ & PUREZZA 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Palosuran hydrochloride (ACT-058362 hydrochloride) 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 hydrochloride can improves pancreatic and renal function in diabetic rats

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. 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. 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. 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 . 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. 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 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).

IC50& Target:IC50: 3.6 nM (human urotensin II receptor)

Specifiche

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

Palosuran hydrochloride (ACT-058362 hydrochloride) 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 hydrochloride can improves

Condizioni di conservazione di stoccaggio

Desiccated,Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Tipo di azione

ANTAGONIST

Nomi e identificatori

PubChem CID

137891318

Peso molecolare

454.99

Domande frequenti

How should this product be stored?

Store at ?80 °C, desiccated. Keep the container tightly closed with desiccant — the material is moisture-sensitive.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2469274-58-4, the molecular formula is C25H31ClN4O2, and the molecular weight is 454.99 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.