TMI 1

TMI 1 C화학적 특성, 용도, 생산

개요

TMI 1 is an inhibitor of disintegrin and metalloproteinase domain-containing protein 17 (ADAM17/TACE; IC₅₀ = 8.4 nM in a cell-free enzyme assay). It inhibits matrix metalloproteinase-1 (MMP-1), -2, -7, -9, -13, and -14, as well as ADAM-TS-4 in vitro (IC₅₀s = 6.6, 4.7, 26, 12, 3, 26, and 100 nM, respectively). It also inhibits ADAM8, -10, -12, and -17/TACE in cell-free enzyme assays with K_i values of 21, 16, 1.8, and 0.079 nM, respectively, with slow-binding inhibition of ADAM17/TACE but not the other ADAM enzymes. TMI 1 inhibits LPS-induced TNF-α secretion in Raw and THP-1 cells (IC₅₀s = 40 and 200 nM, respectively), as well as in isolated human monocytes and whole blood (IC₅₀s = 190 and 300 nM, respectively). It inhibits the production of TNF-α ex vivo in synovium isolated from the inflamed joints of patients with rheumatoid arthritis with IC₅₀ values of less than 100 nM without inhibiting TNF-α expression in vitro. TMI 1 inhibits LPS-induced TNF-α production in mice (ED₅₀ = 5 mg/kg) and reduces disease severity in mouse models of collagen-induced arthritis. It also decreases cell viability of (ED₅₀s = 1.3-8.1 μM), and induces caspase-3/7 activity in, a variety of cancer cell lines and induces tumor apoptosis and reduces tumor growth in an MMTV-ErbB2/neu mouse model of breast cancer when administered at a dose of 100 mg/kg.

용도

TMI 1 is a dual TACE/MMP inhibitor, which represents a unique class of orally bioavailable small molecule TNF inhibitors that may be effective and beneficial for treating rhuematoid arthritis.

TMI 1 준비 용품 및 원자재

원자재

준비 용품

TMI 1 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Nantong HI-FUTURE Biology Co., Ltd.	+undefined18051384581	sales@chemhifuture.com	China	3136	58
TargetMol Chemicals Inc.	+1-781-999-5354	support@targetmol.com	United States	19973	58
Aladdin Scientific	+1-+1(833)-552-7181	sales@aladdinsci.com	United States	57511	58
BOC Sciences	1-631-485-4226; 16314854226	info@bocsci.com	United States	14059	65
Shanghai EFE Biological Technology Co., Ltd.	021-65675885 18964387627	info@efebio.com	China	9708	58
Shanghai Hongye Biotechnology Co. Ltd	400-9205774	sales@glpbio.cn	China	6870	58
ChemeGen(Shanghai) Biotechnology Co.,Ltd.	18818260767	sales@chemegen.com	China	11289	58
Energy Chemical	021-58432009 400-005-6266	marketing@energy-chemical.com	China	44941	58
Nantong Hi-Future Biotechnology Co., Ltd	18051384581	sales@chemhifuture.com	China	3059	58
TargetMol Chemicals Inc.	4008200310	marketing@tsbiochem.com	China	24017	58