TAK-242 #75523

Name: TAK-242
Price: 243.00 USD
Availability: InStock

Product Information

Product Usage Information

TAK-242 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute 5 mg of powder in 1.38 mL of DMSO. Working concentrations and length of treatment can vary depending on the desired effect.

Storage

Store lyophilized at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, store at -20ºC and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight	361.82 g/mol
Purity	>98%
Molecular Formula	C₁₅H₁₇ClFNO₄S
CAS	243984-11-4
Solubility	Soluble in DMSO at 100 mg/mL.

Background

TAK-242 is a small-molecule that specifically inhibits Toll-like receptor 4 signaling through binding to the intracellular domain of TLR4 at Cys747 (1). TLR4 triggers activation of the NF-κB, IRF-3, and MAPK pathways, leading to production of inflammatory cytokines. TAK-242 inhibits binding between TLR4 and adaptor molecules, including Toll/interleukin-1 (IL-1) receptor domain-containing adaptor protein (TIRAP), which blocks activation of NF-κB and other downstream signaling events (2). In LPS-stimulated mouse macrophages, TAK-242 suppressed the production of NO and the inflammatory cytokines tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) (3). In a study of LPS-induced myotube atrophy, TAK-242 provides a protective effect by inhibiting TLR4 and suppressing TNF-α- and IL-6-mediated inflammatory responses. Similar results were seen in a mouse model of endotoxemia, with TAK-242 inhibiting activation of inflammatory and proteolytic pathways and reversing the muscle wasting impact induced by LPS treatment (4).

Limited Uses

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For Research Use Only. Not For Use In Diagnostic Procedures.

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