M-62812 | CAS# 613263-00-6 (HCl) | TLR4 inhibitor

MedKoo Cat#: 574805 | Name: M-62812

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

M-62812 is a TLR4 inhibitor that inhibits LPS-induced NF-κB activation in HEK293 cells and LPS-induced cytokine production and procoagulant effects in PBMCs and HUVECs.

Chemical Structure

M-62812

CAS# 613263-00-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 574805

Name: M-62812

CAS#: 613263-00-6 (HCl)

Chemical Formula: C13H13Cl2N3OS

Exact Mass: 329.0156

Molecular Weight: 330.23

Elemental Analysis: C, 47.28; H, 3.97; Cl, 21.47; N, 12.72; O, 4.84; S, 9.71

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 350.00	2 Weeks
50mg	USD 950.00	2 Weeks

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Related CAS #

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Synonym

M-62812; M62812; M 62812

IUPAC/Chemical Name

6-(2-Aminophenoxy)-1,2-benzisothiazol-3-amine dihydrochloride

InChi Key

SMTKPLISDFNJDJ-UHFFFAOYSA-N

InChi Code

InChI=1S/C13H11N3OS.2ClH/c14-10-3-1-2-4-11(10)17-8-5-6-9-12(7-8)18-16-13(9)15;;/h1-7H,14H2,(H2,15,16);2*1H

SMILES Code

NC1=NSC2=C1C=CC(OC3=CC=CC=C3N)=C2.[H]Cl.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

M-62812 is a TLR4 inhibitor.

In vitro activity:

This study found a new benzisothiazole derivative, M62812 that inhibits TLR4 signal transduction. This compound suppressed LPS-induced upregulation of inflammatory cytokines, adhesion molecules and procoagulant activity in human vascular endothelial cells and peripheral mononuclear cells. The half maximal inhibitory concentrations in these assays ranged from 1 to 3 microg/ml. Reference: Eur J Pharmacol. 2007 Aug 27;569(3):237-43. https://pubmed.ncbi.nlm.nih.gov/17588563/

In vivo activity:

Single intravenous administration of M62812 (10-20 mg/kg) protected mice from lethality and reduced inflammatory and coagulatory parameters in a murine d-galactosamine-sensitized endotoxin shock model. M62812 (20 mg/kg) also prevented mice from lethality in a murine cecal ligation and puncture model. These results suggest that inhibition of TLR4 signal transduction can suppress coagulation as well as inflammation during sepsis and may be clinically beneficial in sepsis treatment. Reference: Eur J Pharmacol. 2007 Aug 27;569(3):237-43. https://pubmed.ncbi.nlm.nih.gov/17588563/

	Solvent	mg/mL	mM
Solubility
	DMSO	16.5	50.00
	Water	33.0	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

Nakamura M, Shimizu Y, Sato Y, Miyazaki Y, Satoh T, Mizuno M, Kato Y, Hosaka Y, Furusako S. Toll-like receptor 4 signal transduction inhibitor, M62812, suppresses endothelial cell and leukocyte activation and prevents lethal septic shock in mice. Eur J Pharmacol. 2007 Aug 27;569(3):237-43. doi: 10.1016/j.ejphar.2007.05.013. Epub 2007 Jun 5. PMID: 17588563.

In vitro protocol:

In vivo protocol:

1. 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