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Merck
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B2186

Sigma-Aldrich

BL-1249

≥98% (HPLC)

Sinonimo/i:

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

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10 MG
CHF 235.00
50 MG
CHF 935.00

CHF 235.00


Spedizione prevista il02 giugno 2025


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Cambia visualizzazione
10 MG
CHF 235.00
50 MG
CHF 935.00

About This Item

Formula empirica (notazione di Hill):
C17H17N5
Numero CAS:
Peso molecolare:
291.35
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77

CHF 235.00


Spedizione prevista il02 giugno 2025


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Livello qualitativo

Saggio

≥98% (HPLC)

Stato

solid

Condizioni di stoccaggio

protect from light

Colore

pink to brown

Solubilità

DMSO: ~17.5 mg/mL
H2O: insoluble

Temperatura di conservazione

−20°C

Stringa SMILE

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)
YYNRZIFBTOUICE-UHFFFAOYSA-N

Descrizione generale

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

Applicazioni

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]

Azioni biochim/fisiol

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.

Caratteristiche e vantaggi

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.

Pittogrammi

Exclamation mark

Avvertenze

Warning

Indicazioni di pericolo

Classi di pericolo

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

Organi bersaglio

Respiratory system

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Dispositivi di protezione individuale

dust mask type N95 (US), Eyeshields, Gloves


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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 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
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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