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B2186

Sigma-Aldrich

BL-1249

≥98% (HPLC)

Sinônimo(s):

(5,6,7,8-Tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine

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10 MG
R$ 2.195,00
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About This Item

Fórmula empírica (Notação de Hill):
C17H17N5
Número CAS:
18200-13-0
Peso molecular:
291.35
Número MDL:
MFCD08276915
Código UNSPSC:
12352200
ID de substância PubChem:
24724415
NACRES:
NA.77

R$ 2.195,00

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Nível de qualidade

100

Ensaio

≥98% (HPLC)

Formulário

solid

condição de armazenamento

protect from light

cor

pink to brown

solubilidade

DMSO: ~17.5 mg/mL
H2O: insoluble

temperatura de armazenamento

−20°C

cadeia de caracteres SMILES

C1CCc2c(C1)cccc2Nc3ccccc3-c4nnn[nH]4

InChI

1S/C17H17N5/c1-2-8-13-12(6-1)7-5-11-15(13)18-16-10-4-3-9-14(16)17-19-21-22-20-17/h3-5,7,9-11,18H,1-2,6,8H2,(H,19,20,21,22)

chave InChI

YYNRZIFBTOUICE-UHFFFAOYSA-N

Descrição geral

BL-1249 is a non-steroid anti-inflammatory drug and an inhibitor of the cyclooxygenase (COX) enzyme.[1]

Aplicação

BL-1249 has been used:
  • as an activator of mechano-gated K2P channel in contracted mouse ileum and colon tissues[1]
  • as a TWIK related potassium channel (TREK2) modulator and in U-2 OS osteosarcoma cell line[2]
  • as a TREK1 and TREK2 activator in mice.[3]

Ações bioquímicas/fisiológicas

BL-1249 also activates TWIK related potassium channel 2 (TREK2). It interacts with K2P channel at the negatively charged activator site and modulates channel opening.[4]
BL-1249 is a potassium TREK-1 channel activator.
BL-1249 is a putative activator of potassium TREK-1 channel.

Características e benefícios

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pictogramas

Exclamation mark
GHS07

Palavra indicadora

Warning

Frases de perigo

H315,H319,H335,H413

Declarações de precaução

P273 - P302 + P352 - P305 + P351 + P338

Classificações de perigo

Aquatic Chronic 4 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Órgãos-alvo

Respiratory system

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Equipamento de proteção individual

dust mask type N95 (US), Eyeshields, Gloves

Escolha uma das versões mais recentes:

Certificados de análise (COA)

Lot/Batch Number
0000415588
0000415588
0000392833
0000392833
0000240334

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Visite a Biblioteca de Documentos

Ruolin Ma et al.
Frontiers in pharmacology, 11, 434-434 (2020-04-23)
TREK-1 channel activity is a critical regulator of neuronal, cardiac, and smooth muscle physiology and pathology. The antidepressant peptide, spadin, has been proposed to be a TREK-1-specific blocker. Here we sought to examine the mechanism of action underlying spadin inhibition
Ehab Al-Moubarak et al.
Scientific reports, 9(1), 12394-12394 (2019-08-29)
A better understanding of the gating of TREK two pore domain potassium (K2P) channels and their activation by compounds such as the negatively charged activator, flufenamic acid (FFA) is critical in the search for more potent and selective activators of
Ruolin Ma et al.
Frontiers in physiology, 9, 157-157 (2018-03-23)
Gastrointestinal (GI) motility disorders such as irritable bowel syndrome (IBS) can occur when coordinated smooth muscle contractility is disrupted. Potassium (K+) channels regulate GI smooth muscle tone and are key to GI tract relaxation, but their molecular and functional phenotypes
Svetlana Tertyshnikova et al.
The Journal of pharmacology and experimental therapeutics, 313(1), 250-259 (2004-12-21)
BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine] produced a concentration-dependent membrane hyperpolarization of cultured human bladder myocytes, assessed as either a reduction in fluorescence of the voltage-sensitive dye bis-(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 = 1.26 +/- 0.6 microM) or by direct electrophysiological measurement (EC50 = 1.49
Paul D Wright et al.
Biochemical and biophysical research communications, 520(1), 35-40 (2019-10-01)
TREK2 (KCNK10, K2P10.1) is a two-pore domain potassium (K2P) channel and a potential target for the treatment of pain. Like the majority of the K2P superfamily, there is currently a lack of useful pharmacological tools to study TREK2. Here we

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