Pranlukast - Moligand™, 10mM in DMSO , Cysteinyl leukotriene receptor 1 antagonist, CAS No.103177-37-3, Cysteinyl leukotriene receptor 1 antagonist

CAS: 103177-37-3 Cat. No.: P408556 Fórmula: C₂₇H₂₃N₅O₄ Peso molecular: 481.5 Número CE: 808-178-9

GRAU & PUREZA Moligand™, 10mM in DMSO

Synonyms

ONO-1078 | N-​[4-​oxo-​2-​(2H-​tetrazol-​5-​yl)​-​4H-​1-​benzopyran-​8-​yl]​-​4-​(4-​phenylbutoxy)​-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

Pranlukast Pranlukast (ONO-1078) is an orally administered, and selective antagonist of the cysteinyl leukotrienes (LT) C(4), LTD(4) and LTE(4), used in the prophylactic treatment of chronic bronchial asthma.
In vitro

Pranlukast inhibits NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells by about 40% & 30%, respectively. Pranlukast and MK-571 inhibit NF-kappa B activation in 1.3% DMSO-differentiated U-937 and Jurkat cells in a dose-related manner. Pranlukast and MK-571 inhibits LPS-induced IL-6 production in PBMC by about 65% and 15%, respectively. Pranlukast or zafirlukast significantly inhibits 10 mM LTD4-evoked 35SO4 output in a concentration-dependent fashion, with maximal inhibitions of 83% at 10 mM Pranlukast and 78% at 10 mM Zafirlukast, and IC50 values of 0.3 mM for Pranlukast and 0.6 mM for Zafirlukast. Pranlukast (0.5 microM) causes a parallel rightward shift of the LTD4 concentration-response curve with a pKB of 7. Pranlukast or Zafirlukast (5 microM each) significantly suppresses ovalbumin-induced secretion in tracheae from sensitized guinea-pigs by 70% and 65%, respectively. Pranlukast also inhibits NF-kappaB activation induced by phorbol 12-myristate 13-acetate (PMA). Pranlukast also significantly inhibits LPS-induced MUC2 mRNA expression by reverse transcription-polymerase chain reaction (RT-PCR) analysis in NCI-H292 cells. Pranlukast also inhibits LPS-induced MUC2 gene expression in HM3-MUC2 cells.

In vivo

Pranlukast significantly reduces lesion volume, and increases neuron densities in the cortex and hippocampal CA1 region in the ischemic hemispheres of mice. Pranlukast also remarkably reduces the thickness of a scar wall in the ischemic hemispheres of mice.
Cell Data

cell lines：Oocytes

Concentrations：

Incubation Time：

Powder Purity:≥99%

Especificações

Sinónimos

ONO-1078 | N-​[4-​oxo-​2-​(2H-​tetrazol-​5-​yl)​-​4H-​1-​benzopyran-​8-​yl]​-​4-​(4-​phenylbutoxy)​-benzamide

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

Pranlukast (ONO-1078) is an orally administered, and selective antagonist of the cysteinyl leukotrienes (LT) C(4), LTD(4) and LTE(4), used in the prophylactic treatment of chronic bronchial asthma.

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.

Grau

Moligand™

Tipo de ação

ANTAGONIST

Mecanismo de ação

Cysteinyl leukotriene receptor 1 antagonist

Propriedades do produto

ALogP

4.2

Nomes e identificadores

SMILES isoméricas

C1=CC=C(C=C1)CCCCOC2=CC=C(C=C2)C(=O)NC3=CC=CC4=C3OC(=CC4=O)C5=NNN=N5

CAS alternativo

103177-37-3；150821-03-7

Termos de entrada MeSH

8-(4 (4-phenylbutoxy)benzoyl)amino-2-(tetrazol-5'-yl)-4-oxo-4H-1-benzopyran;ONO 1078;ONO-1078;ONO-RS 411;ONO-RS-411;pranlukast;SB 205312

Peso molecular

481.5

Reaxy-Rn

26251743

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26251743&ln=

Alvos associados (humanos)

CYSLTR2 Tchem Cysteinyl leukotriene receptor 2 (2 Activities)

Discover Target: CYSLTR2

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

CYSLTR1 Tclin Cysteinyl leukotriene receptor 1 (4 Activities)

Discover Target: CYSLTR1

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

Propriedades químicas e físicas

• Ponto de fusão (°C): 233 °C