BAY-1316957 - 10mM in DMSO , CAS No.1613264-40-6

CAS: 1613264-40-6 Cat. No.: B654960 Fórmula: C₂₇H₂₇N₃O₃ Peso molecular: 441.52 PubChem CID: 90202558

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC 50 of 15.3 nM for human EP4-R . BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research

In Vitro

BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BAY-1316957 (Compound 32; 0.2-5 mg/kg; oral administration; once) treatment significantly reduces mechanical allodynia in dmPGE2 pain model . The pharmacokinetic parameters of BAY-1316957 (Compound 32) shows a low clearance, long half-life, and high bioavailability (F%=90%) in Wistar rats. Investigation of the metabolic pathways of BAY-1316957 (Compound 32) in human, rat, mouse, dog, and monkey hepatocytes revealed that the formation of the acyl glucuronide was also the common and predominant route of biotransformation, mainly catalyzed by UGT1A1 and to a lesser extent by UGT1A3 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male adult Sprague Dawley rats (220-265 g) injected with 16,16-dimethyl prostaglandin E2 (dmPGE2) Dosage: 0.2 mg/kg, 1 mg/kg, 5 mg/kg Administration: Oral administration; once Result: Significantly reduced paw withdrawal thresholds in dmPGE2 pain model.

IC50& Target:human EP4-R 15.3 nM (IC 50 )

Specifications

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC 50 of 15.3 nM for human EP4-R . BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometr

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

ANTAGONIST

Nomes e identificadores

SMILES isoméricas

CCN1C2=C(C=C(C=C2)C)C3=C1C=CC(=C3)C4=NC5=C(N4CCOC)C=CC(=C5C)C(=O)O

PubChem CID

90202558

Peso molecular

441.52

Alvos associados (humanos)

PTGER4 Tclin Prostaglandin E2 receptor EP4 subtype (1 Activities)

Discover Target: PTGER4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)