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B2186

Sigma-Aldrich

BL-1249

≥98% (HPLC)

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C17H17N5
Numéro CAS:
18200-13-0
Poids moléculaire :
291.35
Numéro MDL:
MFCD08276915
Code UNSPSC :
12352200
ID de substance PubChem :
24724415
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Essai

≥98% (HPLC)

Forme

solid

Conditions de stockage

protect from light

Couleur

pink to brown

Solubilité

DMSO: ~17.5 mg/mL
H2O: insoluble

Température de stockage

−20°C

Chaîne 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)

Clé InChI

YYNRZIFBTOUICE-UHFFFAOYSA-N

Description générale

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

Application

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

Actions biochimiques/physiologiques

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.
BL-1249 is a putative activator of potassium TREK-1 channel.

Caractéristiques et avantages

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.

Pictogrammes

Exclamation mark
GHS07

Mention d'avertissement

Warning

Mentions de danger

H315,H319,H335,H413

Classification des risques

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

Organes cibles

Respiratory system

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

dust mask type N95 (US), Eyeshields, Gloves

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Certificats d'analyse (COA)

Lot/Batch Number
0000392833
0000392833
0000240334
096M4618V
063M4619V

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Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

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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Potassium Channels

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Potassium Channels

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