티스토리 뷰

안녕하세요!

TargetMol (Target molecule Corp.) 공식 수입/공급 업체 코아사이언스 입니다.

 

자세한 상품 정보 및 관련 문의는 전화 02-858-0328 또는 info@coresciences.co.kr로 문의주시기 바랍니다.

감사합니다!

 

Resatorvid

=CLI-095, TAK-242

Cat.# TQ0181 / Size: 1mg, 2mg, 5mg, 10mg, 25mg, 50mg, 100mg

Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.

Biological Description

Description
Resatorvid (TAK-242) is a selective inhibitor of Toll-like receptor 4 (TLR4). Resatorvid binds directly to Cys747 and prevents TLR4 from binding to TIRAP, thereby blocking downstream signaling. Resatorvid has antitumor activity, anti-inflammatory activity, and neuroprotective effects.
Targets&IC50
TNF R:1.9 nM , IL-6:1.3 nM , NO:1.8 nM
In vitro
METHODS: Breast cancer cell lines MCF7, SKBR3, MDA-MB-231 and BT-474 were treated with Resatorvid (10-150 µM) for 48 h. Cell viability was measured using MTT Assay.
RESULTS: Resatorvid dose-dependently inhibited the viability of breast cancer cell lines. [1]
METHODS: Macrophage RAW264.7 was treated with Resatorvid (1-100 nM) and LPS (5 ng/mL), IFN-γ (1 U/mL) for 4 h. Gene expression levels were measured by RT-qPCR.
RESULTS: Resatorvid inhibited LPS and IFN-γ induced mRNA expression of IL-6 and TNF-α in RAW264.7 cells. [2]
In vivo
METHODS: To test the effects on cancer-comorbid depression (BCCD), Resatorvid (3 mg/kg) was administered intraperitoneally to BALB/c mice in the BCCD model once daily for three weeks.
RESULTS: Resatorvid attenuated the symptoms of BCCD mice in vivo.Resatorvid inactivated inflammatory factors and TLR4/NF-κB/NLRP3 signaling pathway in vivo. [3]
METHODS: To investigate the effects on temporomandibular joint osteoarthritis (TMJOA), Resatorvid (10 mg/kg) was injected intraperitoneally twice weekly for four weeks into a CFA-induced TMJOA model in C57BL/6 mice.
RESULTS: Prophylactic treatment with Resatorvid attenuated TMJOA pathology by inhibiting chondrocyte focal prolapse and degeneration, and ROS-induced macrophage inflammation via TLR4/MyD88/NF-κB/NLRP3. [4]
Cell Research
Cell Line: RAW264.7 cells. Concentration: 1 nM, 10 nM, 100 nM. Incubation Time: 4 hours [1]
Animal Research
Animal Model: 30 ApoE knockout and 30 wild-type mice on a C57BL/6 background (female, 10 weeks old). Dosage: 0.3?mg/kg. Administration: i.p.; twice a week; for 4 weeks [3]

Chemical Properties

Synonyms
CLI-095, TAK-242
Molecular Weight
361.82
Formula
C15H17ClFNO4S
CAS No.
243984-11-4

* 본 상품은 오직 연구용으로만 사용 가능합니다. 인체 및 제품화에 사용하실 수 없습니다.

코아사이언스 coresciences Target molecule Corp TargetMol USA distributor Korea 한국 대리점