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B2186

Sigma-Aldrich

BL-1249

≥98% (HPLC)

Synonym(e):

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

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CHF 250.00
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CHF 994.00

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Voraussichtliches Versanddatum29. Mai 2025

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10 MG
CHF 250.00
50 MG
CHF 994.00

About This Item

Empirische Formel (Hill-System):
C17H17N5
CAS-Nummer:
18200-13-0
Molekulargewicht:
291.35
MDL-Nummer:
MFCD08276915
UNSPSC-Code:
12352200
PubChem Substanz-ID:
24724415
NACRES:
NA.77

CHF 250.00

Voraussichtliches Versanddatum29. Mai 2025

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Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

solid

Lagerbedingungen

protect from light

Farbe

pink to brown

Löslichkeit

DMSO: ~17.5 mg/mL
H2O: insoluble

Lagertemp.

−20°C

SMILES String

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)

InChIKey

YYNRZIFBTOUICE-UHFFFAOYSA-N

Verwandte Kategorien

Allgemeine Beschreibung

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

Anwendung

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]

Biochem./physiol. Wirkung

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.

Leistungsmerkmale und Vorteile

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.

Piktogramme

Exclamation mark
GHS07

Signalwort

Warning

Gefahreneinstufungen

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

Zielorgane

Respiratory system

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Persönliche Schutzausrüstung

dust mask type N95 (US), Eyeshields, Gloves

Hier finden Sie alle aktuellen Versionen:

Analysenzertifikate (COA)

Lot/Batch Number
0000415588
0000415588
0000392833
0000392833
0000240334

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Die Dokumentenbibliothek aufrufen

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
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
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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