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614310

Sigma-Aldrich

TLR3/dsRNA Complex Inhibitor

The TLR3/dsRNA Complex Inhibitor blocks dsRNA binding to TLR3.

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Synonym(s):
TLR3/dsRNA Complex Inhibitor, ( R)-2-(3-Chloro-6-fluorobenzo[b]thiophene-2-carboxamido)-3-phenylpropanoic acid, Toll-Like Receptor 3/Double Strand RNA Complex Inhibitor, (R)-2-(3-Chloro-6-fluorobenzo[b]thiophene-2-carboxamido)-3-phenylpropanoic acid, Toll-Like Receptor 3/Double Strand RNA Complex Inhibitor
Empirical Formula (Hill Notation):
C18H13ClFNO3S
Molecular Weight:
377.82

Quality Level

assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 50 mg/mL

shipped in

wet ice

storage temp.

2-8°C

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TLR3/dsRNA Complex Inhibitor

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manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

assay

≥99% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

shipped in

wet ice

shipped in

ambient

shipped in

ambient

shipped in

wet ice

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

2-8°C

General description

A thiophenecarboxamidopropionate compound that acts as a direct, competitive and high affinity inhibitor of dsRNA binding to TLR3 (Ki = 2.96 µM; Kd = 19 nM for dsRNA binding to TLR3) and selectively antagonizes stimulated TLR3 signaling without affecting TLR1/2, TLR2/6, TLR4 and TLR7 pathways. Shown to efficiently repress TNF-α and IL-1β (IC90 = 27 µM) and NO production (IC50 = 3.44 µM) in Poly(I:C)-induced RAW 264.7 macrophages. Exhibits minimal cytotoxicity (IC50 >>100 µM in RAW 264.7 cells) and is weakly active against a panel of 12-representative kinases and 4-cytochrome enzymes (in vitro assays).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Cheng, K., et al. 2011. J. Am. Chem. Soc.133, 3764.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable


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