Przejdź do zawartości
Merck
Wszystkie zdjęcia(1)

Kluczowe dokumenty

614316

Sigma-Aldrich

TAK-242

≥98% (HPLC), solid, TLR4 inhibitor, Calbiochem®

Synonim(y):

Etylo-(6 R)-6-(N-(2-chloro-4-fluorofenylo)sulfamoilo)cykloheks-1-en-1-karboksylan

Zaloguj sięWyświetlanie cen organizacyjnych i kontraktowych
Wszystkie zdjęcia(1)

About This Item

Wzór empiryczny (zapis Hilla):
C15H17ClFNO4S
Numer CAS:
243984-11-4
Masa cząsteczkowa:
361.82
Numer MDL:
MFCD11046362
Kod UNSPSC:
12352200
NACRES:
NA.77

Nazwa produktu

TLR4 Inhibitor, TAK-242, TAK-242; CAS 243984-11-4; is a cell-permeable compound that selectively binds to Cys747 of TLR4 and selectively disrupts its interaction with adaptor molecules TIRAP and TRAM.

Poziom jakości

100

Próba

≥98% (HPLC)

Formularz

solid

producent / nazwa handlowa

Calbiochem®

warunki przechowywania

OK to freeze
protect from light

kolor

white to yellow-white

rozpuszczalność

DMSO: 100 mg/mL

Warunki transportu

wet ice

temp. przechowywania

2-8°C

ciąg SMILES

Fc1cc(c(cc1)N[S](=O)(=O)[C@@H]2CCCC=C2C(=O)OCC)Cl

InChI

1S/C15H17ClFNO4S/c1-2-22-15(19)11-5-3-4-6-14(11)23(20,21)18-13-8-7-10(17)9-12(13)16/h5,7-9,14,18H,2-4,6H2,1H3/t14-/m1/s1

Klucz InChI

LEEIJTHMHDMWLJ-CQSZACIVSA-N

Opis ogólny

A cell-permeable cyclohexenecarboxylate that disrupts TLR4 interaction with adaptor molecules TIRAP and TRAM by selectively binding to TLR4, but not TLR1-3 or TLR5-10, via TLR4 intracellular Cys747 residue. Shown to effectively inhibit TLR4-mediated signaling events, including LPS-induced NO and inflammatory cytokines production in murine RAW264.7 macrophages (IC50 = 1.8, 1.3, and 1.9 nM, respectively, against NO, IL-6, and TNF-α production), TLR4/TIRAP-dependent NF-κB activity as well as TLR4/TIRAP- and TLR4/TRAM-dependent ISRE activity (IC50<300 nM) in HEK293-hTLR4/MD2-CD14 transfected with either TIRAP or TRAM. When administered at an i.v. dose of 3 mg/kg, TAK-242 is reported to completely prevent LPS- (7 mg/kg, i.p.) induced death in mice in vivo. Complete elimination of septic shock-induced death can be extended to live E. coli-infected mice when co-administered with ceftazidime (3 mg/kg TAK-242 and 20 mg/kg ceftazidime, i.v.).

Działania biochem./fizjol.

Cell permeable: yes
Primary Target
TLR4
Reversible: yes

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Harmful (C)

Rekonstytucja

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 1 year at -70°C. Use only fresh DMSO.

Inne uwagi

Matsunaga, N., et al. 2011. Mol. Pharmacol.79, 34.
Takashima, K., et al. 2009. Br. J. Pharmacol.157, 1250.
Li, M., et al. 2006. Mol. Pharmacol.69, 1288.
Yamada, M., et al. 2005. J. Med. Chem.48, 7457.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Ta strona może zawierać tekst przetłumaczony maszynowo.

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 2

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable

Certyfikaty analizy (CoA)

Poszukaj Certyfikaty analizy (CoA), wpisując numer partii/serii produktów. Numery serii i partii można znaleźć na etykiecie produktu po słowach „seria” lub „partia”.

Masz już ten produkt?

Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.

Odwiedź Bibliotekę dokumentów

Qianqian Zheng et al.
Theranostics, 10(22), 9923-9936 (2020-09-16)
Rationale: Hepatocellular carcinoma (HCC) has been increasingly recognized in nonalcoholic steatohepatitis (NASH) patients. Fibroblast growth factor 21 (FGF21) is reported to prevent NASH and delay HCC development. In this study, the effects of FGF21 on NASH progression and NASH-HCC transition
Tetyana P Buzhdygan et al.
Journal of neuroinflammation, 18(1), 63-63 (2021-03-03)
Synthetic cathinones are a category of psychostimulants belonging to the growing number of designer drugs also known as "Novel Psychoactive Substances" (NPS). In recent years, NPS have gained popularity in the recreational drug market due to their amphetamine-like stimulant effects
Anna Stierschneider et al.
International journal of molecular sciences, 22(17) (2021-09-11)
Augmented Toll-like receptor 4 (TLR4) expression was found in nearly 70% of patients with pancreatic adenocarcinoma, which is correlated with increased tumorigenesis and progression. In this study, we engineered a new light-oxygen-voltage-sensing (LOV) domain-based optogenetic cell line (opto-TLR4 PANC-1) that
Kazuhiro Shiizaki et al.
The Journal of clinical investigation, 131(16) (2021-06-30)
The Western pattern diet is rich not only in fat and calories but also in phosphate. The negative effects of excessive fat and calorie intake on health are widely known, but the potential harms of excessive phosphate intake are poorly
Huanyu Jiang et al.
Frontiers in immunology, 13, 913901-913901 (2022-07-23)
Osteoarthritis (OA) is a deteriorating disease of cartilage tissues mainly characterized as low-grade inflammation of the joint. Innate immune molecule surfactant protein D (SP-D) is a member of collectin family of collagenous Ca2+-dependent defense lectins and plays a vital role
Wyświetl wszystkie powiązane dokumenty

Nasz zespół naukowców ma doświadczenie we wszystkich obszarach badań, w tym w naukach przyrodniczych, materiałoznawstwie, syntezie chemicznej, chromatografii, analityce i wielu innych dziedzinach.

Skontaktuj się z zespołem ds. pomocy technicznej