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E6446 dihydrochloride

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Purity:99.44%

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COA HNMR LCMS

E6446 dihydrochloride

Catalog No. T4068Cas No. 1345675-25-3

E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM.

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Pack Size	Price	Availability
1 mg	$109	In Stock
2 mg	$161	In Stock
5 mg	$321	In Stock
10 mg	$396	In Stock
25 mg	$662	In Stock
50 mg	$943	In Stock
100 mg	$1,280	In Stock
1 mL x 10 mM (in DMSO)	$396	In Stock

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Product Introduction

Bioactivity

Description	E6446 dihydrochloride is a novel synthetic antagonist for nucleic acid-sensing TLRs; potently suppressed DNA stimulation of HEK:TLR9 cells with IC50 of 10 nM.
In vitro	E6446 potently inhibited IL-6 production induced by CpG2216 but was ineffective against induction by the TLR3 ligand poly inosine-cytosine. E6446 showed a modest but consistent superiority over AT791, and both were significantly more potent than hydroxychloroquine. Significantly, 250 nM and 1.25 μM E6446 completely suppressed all of the CpG oligo-induced changes in gene expression [1]. E6446 specifically inhibited TLR9 activation with CpG ODN 2006, in the range of 0.01–0.03 μM. A 100-fold higher concentration (2–8 μM) of E6446 was required to inhibit TLR7/8 activated by the imidazoquinoline compound R848 [2].
In vivo	To test their activity in vivo, mice were orally dosed with 20 mg/kg of AT791 or E6446 and 18 hours later were challenged with 60 μg CpG1668 oligonucleotide injected subcutaneously. CpG1668-induced IL-6 production was inhibited ~50% by AT791 and almost completely by E6446 [1]. therapy with E6446 diminished the activation of TLR9 and prevented the exacerbated cytokine response observed during acute Plasmodium infection [2].

Chemical Properties

Molecular Weight	522.51
Formula	C27H37Cl2N3O3
Cas No.	1345675-25-3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5.22 mg/mL (10 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9138 mL	9.5692 mL	19.1384 mL	95.6919 mL
5 mM	0.3828 mL	1.9138 mL	3.8277 mL	19.1384 mL

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