research use only

E6446 dihydrochloride TLR inhibitor

Name: E6446 dihydrochloride
Brand: Selleck Chemicals
SKU: S6719
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S6719

E6446 dihydrochloride is a specific Toll-like receptor 9 inhibitor.

Chemical Structure

Molecular Weight: 522.51

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 98.99%

98.99

Related Targets	Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX Histamine Receptor TNF-alpha ROS Parasite PD-1/PD-L1 Prostaglandin Receptor IFN CXCR Nrf2 NOS CCR NLRP3 eIF STING AhR IL Receptor NADPH-oxidase Complement System IRAK β-lactamase IDO/TDO PGES FKBP LTR
Related Products	Resatorvid (TAK-242) Resiquimod (R-848) Motolimod Cu-CPT22 Vesatolimod (GS-9620) TLR2-IN-C29 MD2-IN-1 Lipopolysaccharides IRAK4-IN-2 CU-T12-9 E6446 TLR4-IN-C34 Polyinosinic acid-polycytidylic acid (Poly(I:C)) SM 324405 Polyinosinic-polycytidylic acid sodium IAXO-102 CU-CPT 4a CU-CPD107 FSL-1 AT791 1V209 (TLR7 agonist T7) MTT5 Enpatoran Cnidii Fructus Extract TLR4 Antibody [J3D3] Telratolimod Robinin Enpatoran Hydrochloride MD2-TLR4-IN-1 TLR7/8 agonist 1 dihydrochloride

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HEK293	Function assay	24 hrs	Antagonist activity at human TLR9 expressed in HEK293 cells assessed as inhibition of CpGB-induced NF-kappaB activation after 24 hrs by spectrophotometry based SEAP reporter gene assay, IC50=0.015μM	28437629
plasmacytoid dendritic cells	Function assay	18 hrs	Antagonist activity at TLR9 in human plasmacytoid dendritic cells assessed as inhibition of CpGA-induced IFN-alpha production after 18 hrs by ELISA, IC50<0.05μM	28437629
HEK293	Function assay	24 hrs	Antagonist activity at human TLR7 expressed in HEK293 cells assessed as inhibition of CL264-induced NF-kappaB activation after 24 hrs by spectrophotometry based SEAP reporter gene assay, IC50=1.99μM	28437629
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	522.51	Formula	C₂₇H₃₇Cl₂N₃O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1345675-25-3	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CCN(C1)CCCOC2=CC=C(C=C2)C3=NC4=C(O3)C=C(C=C4)OCCCN5CCCC5.Cl.Cl

Solubility

In vitro
Batch:

Water : 100 mg/mL

DMSO : 3 mg/mL (5.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.48mM)
	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.250mg/ml (0.48mM)
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	TLR9 ^[1]
In vivo	E6446 is orally bioavailable (20%) and has high volumes of distribution in mice (95.9 l/kg)^[1].
References	[1] https://pubmed.ncbi.nlm.nih.gov/24342772/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):