BMS-986224 - ≥98% , CAS No.2055200-88-7

CAS: 2055200-88-7 Cat. No.: B648552 Formula: C₂₄H₂₃ClN₄O₆ Peso molecolare: 498.92 PubChem CID: 137106310

QUALITÀ & PUREZZA ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

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.

Form:Solid

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

Specifiche

Specifiche e purezza

≥98%

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 -20°C

Spedito in

Ice chest + Ice pads

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

Purezza

≥98%

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

Obiettivi associati (non umani)

Aplnr Apelin receptor (201 Activities)

Discover Target: Aplnr

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Meccanismi d'azione

Proprietà chimiche e fisiche

• Solubilità: DMSO : 20.83 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)