BL-1249 Struktur

BL-1249

Bezeichnung:BL-1249

CAS-Nr18200-13-0

Englisch Name:BL-1249

CBNumberCB4503185

SummenformelC17H17N5

Molgewicht291.35

MOL-Datei18200-13-0.mol

BL-1249 physikalisch-chemischer Eigenschaften

Siedepunkt	492.6±55.0 °C(Predicted)
Dichte	1.291±0.06 g/cm3(Predicted)
storage temp.	-20°C
Löslichkeit	DMSO: ~17.5mg/mL
Aggregatzustand	solid
pka	4.10±0.10(Predicted)
Farbe	pink to brown

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-37/39
WGK Germany	3

Gefahreninformationscode (GHS)

BL-1249 Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
Verwenden
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.
Allgemeine Beschreibung
BL-1249 is a non-steroid anti-inflammatory drug and an inhibitor of the cyclooxygenase (COX) enzyme.
Biologische Aktivität
[(5, 6, 7, 8-tetrahydro-naphthalen-1-yl)-[2-(1h-tetrazol-5-yl)-phenyl]-amine], named bl 1249, is a putative potassium channel opener with bladder-relaxant properties. in cultured bladder smooth muscle cells, bl 1249 decreased dibac4 (3) fluorescence in a concentration-dependent manner with an ec50 of 1.26 ± 0.6 μm. in human bladder cells, bl 1249 resulted in hyperpolarization in a concentration-dependent manner and yielded an ec50 of 1.49±0.08 μm. bl 1249 relaxed 30 mm kcl precontracted bladder strips in a concentration-dependent manner and yielded an ec50 of 1.1 ± 0.37 μm [1].there are several types of potassium channels in urinary bladder myocytes and they are important in determining contractility and excitability of bladder smooth muscle. these channels include maxi-k+, katp, members of the voltage-gated kv family, sk family and, possibly, members of the kcnq family. open potassium channels can increase potassium efflux from the cell and produce membrane potential hyperpolarization, thereby decrease the activation of voltage-dependent calcium channels [1].in human bladder myocytes, bl 1249 produced large instantaneously non-inactivating, activating outward currents that were readily reversible following drug washout. the bl 1249-induced current was hence of a reversal potential of near -80 mv under the physiological k+ gradient, this indicated that the current is carried by k+ ions [1].in anesthetized rats, bl 1249 at a concentration of 1 mg/kg significantly decreased (p< 0.01) micturition contractions during the 15-min period immediately following dosing; for the 15- to 30-min period, the decrease was significant but less (p< 0.05). administration of bl 1249 at a concentration of 1 mg/kg had no effect on mean arterial blood pressure (mabp) during the 0- to 15-min period immediately following administration. during the 15- to 30-min period, bl 1249 administration increased mabp by less than 10% [1].
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.
Lager
Store at -20°C
Einzelnachweise
[1]. svetlana tertyshnikova, ronald j. knox, mary jane plym, et al. bl-1249 [(5, 6, 7, 8-tetrahydro-naphthalen-1-yl)-[2-(1h-tetrazol-5-yl)-phenyl]-amine]: a putative potassium channel opener with bladder-relaxant properties. the journal of pharmacology and experimental therapeutics, 2015, 313(1):250-259.

BL-1249 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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