BMS-986224 - 10mM in DMSO , CAS No.2055200-88-7

CAS: 2055200-88-7 Cat. No.: B655474 Formula: C₂₄H₂₃ClN₄O₆ Peso molecolare: 498.92 PubChem CID: 137106310

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

BMS-986224 is a potent, selective and orally active APJ receptor agonist ( K d = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1 ) apelin-13. BMS-986224 has the potential for the research of heart failure

In Vitro

BMS-986224 fully inhibits forskolin-mediated cAMP production, with an EC 50 for human APJ of 0.02 nM. BMS-986224 (0-100 nM) fully stimulates β-arrestin recruitment, ERK phosphorylation, and APJ internalization in Chinese hamster ovary-K1 or HEK293 ZF cells. BMS-986224 is a potent and selective APJ receptor agonist that exhibits a similar signaling profile to (Pyr1) apelin-13. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BMS-986224 (0.192 mg/kg or 3 mg/kg; SC infusion; daily;) in the RHR model increased stroke volume and cardiac output to levels seen in healthy animals but without preventing cardiac hypertrophy and fibrosis, effects differentiated from enalapril . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (renal hypertensive rat model) Dosage: 0.192 mg/kg or 3 mg/kg Administration: SC infusion; daily; Initiated 3 days before surgery and continued for 7 days after surgery Result: The achieved steady-state plasma concentrations during 10-day infusion were 102 and 2686 nmol/L at low dose and HD, respectively. At the low dose, BMS-986224 increased SV and CO without affecting other measured parameters, including the measured diastolic parameters, cardiac fibrosis, and heart weight in RHR.

IC50& Target:Kd: 0.3 nM (APJ receptor)

Specifications

Specifiche e purezza

10mM in DMSO

Meccanismi biochimici e fisiologici

BMS-986224 is a potent, selective and orally active APJ receptor agonist ( K d = 0.3 nM). BMS-986224 exhibits similar receptor binding and signaling profile to (Pyr 1 ) apelin-13. BMS-986224 has the potential for the research of heart failure.

Condizioni di conservazione di stoccaggio

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.

Nomi e identificatori

• Isomeri SMILES: CCOCC1=C(C(=C(C(=O)N1)C2=NN=C(O2)CC3=NC=C(C=C3)Cl)O)C4=C(C=CC=C4OC)OC
• PubChem CID: 137106310
• Peso molecolare: 498.92

Domande frequenti

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

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 2055200-88-7, the molecular formula is C24H23ClN4O6, and the molecular weight is 498.92 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.