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Description: TLR-4 inhibitor
Chemical Name: 6-(2-Aminophenoxy)-1,2-benzisothiazol-3-amine dihydrochloride
Purity: ≥98% (HPLC)
Citations (2)
Reviews (1)
Pathways (1)

Biological Activity for M62812

M62812 is a TLR4 inhibitor. Inhibits LPS-induced NF-κB activation in HEK293 cells (IC50 = 2.4 μg/mL). Also inhibits LPS-induced cytokine production and procoagulant effects in PBMCs and HUVECs. Prolongs survival in a mouse septic shock model.

Compound Libraries for M62812

M62812 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for M62812

M. Wt 330.23
Formula C13H11N3OS.2HCl
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 613263-00-6
PubChem ID 44224214
Smiles NC1=CC=CC=C1OC2=CC=C3C(SN=C3N)=C2.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for M62812

Solvent Max Conc. mg/mL Max Conc. mM
water 33.02 100
DMSO 16.51 50

Preparing Stock Solutions for M62812

The following data is based on the product molecular weight 330.23. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.03 mL 15.14 mL 30.28 mL
5 mM 0.61 mL 3.03 mL 6.06 mL
10 mM 0.3 mL 1.51 mL 3.03 mL
50 mM 0.06 mL 0.3 mL 0.61 mL

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References for M62812

References are publications that support the biological activity of the product.

Nakamura et al (2007) Toll-like receptor 4 signal transduction inhibitor, M62812, suppresses endothelial cell and leukocyte activation and prevents lethal septic shock in mice. Eur.J.Pharmacol. 569 237 PMID: 17588563

If you know of a relevant reference for M62812, please let us know.

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Keywords: M62812, M62812 supplier, Toll-like, receptors, inhibits, inhibitors, TLR-4, sepsis, septic, shock, Receptors, 5705, Tocris Bioscience

2 Citations for M62812

Citations are publications that use Tocris products. Selected citations for M62812 include:

Nara et al (2020) TAP2, a peptide antagonist of Toll-like receptor 4, attenuates pain and cartilage degradation in a monoiodoacetate-induced arthritis rat model. Sci Rep 10 17451 PMID: 33060735

Jing et al (2020) Mucosal Vaccination for Influenza Protection Enhanced by Catalytic Immune-Adjuvant. Adv Sci (Weinh) 7 2000771 PMID: 32999833

Do you know of a great paper that uses M62812 from Tocris? Please let us know.

Reviews for M62812

Average Rating: 3 (Based on 1 Review.)

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Ok, needs titrations.
By Scott Scarneo on 02/06/2019
Assay Type: Ex Vivo
Species: Mouse
Cell Line/Tissue: THP-1

We were interested in looking at LPS TLR4 mediated signaling and were hoping to use this to block this.

review image

Pathways for M62812

Toll-like Receptor Signaling Pathway

Toll-like Receptor Signaling Pathway

TLR signaling is involved in the cellular response to threatening molecules such as bacteria and viruses. It results in an inflammatory and immmunological response.