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Merck

B2186

BL-1249

≥98% (HPLC)

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C17H17N5
CAS Number:
18200-13-0
Molecular Weight:
291.35
NACRES:
NA.77
PubChem Substance ID:
24724415
UNSPSC Code:
12352200
MDL number:
MFCD08276915

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Product Name

BL-1249, ≥98% (HPLC)

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)

SMILES string

C1CCc2c(C1)cccc2Nc3ccccc3-c4nnn[nH]4

InChI key

YYNRZIFBTOUICE-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

storage condition

protect from light

color

pink to brown

solubility

DMSO: ~17.5 mg/mL
H2O: insoluble

storage temp.

−20°C

Quality Level

100

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This Item
236005SML2015182690
BL-1249 ≥98% (HPLC)

Sigma-Aldrich

B2186

BL-1249

COX-1 Inhibitor, FR122047 The COX-1 Inhibitor, FR122047, also referenced under CAS 130717-51-0, controls the biological activity of COX-1. This small molecule/inhibitor is primarily used for Cell Signaling applications.

Sigma-Aldrich

236005

COX-1 Inhibitor, FR122047

MM11253 ≥98% (HPLC)

Sigma-Aldrich

SML2015

MM11253

AhR Agonist V, VAF347 The AhR Agonist V, VAF347 controls the biological activity of AhR. This small molecule/inhibitor is primarily used for Biochemicals applications.

Sigma-Aldrich

182690

AhR Agonist V, VAF347

form

solid

form

solid

form

powder

form

solid

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥99% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

-

Quality Level

100

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: ~17.5 mg/mL, H2O: insoluble

solubility

1 M HCl: 2 mg/mL, water: 4 mg/mL, DMSO: 5 mg/mL

solubility

DMSO: 2 mg/mL, clear

solubility

DMSO: 50 mg/mL

storage condition

protect from light

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

storage condition

-

storage condition

OK to freeze, protect from light

Application

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 Actions

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.

Features and Benefits

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.

General description

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

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

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

target_organs

Respiratory system

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

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Certificates of Analysis (COA)

Lot/Batch Number
0000415588
0000415588
0000392833
0000392833
0000240334

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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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