S1697
SPD304
≥98% (HPLC), solid
동의어(들):
6,7-Dimethyl-3-[[methyl[2-[methyl[[1-[3-(trifluoromethyl)phenyl]-1H-indol-3-yl]methyl]amino]ethyl]amino]methyl]-(4H-1-Benzopyran-4-one dihydrochloride, SPD00000304
로그인조직 및 계약 가격 보기
모든 사진(1)
About This Item
실험식(Hill 표기법):
C32H32F3N3O2 · 2HCl
CAS Number:
Molecular Weight:
620.53
MDL number:
UNSPSC 코드:
51111800
PubChem Substance ID:
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
양식
solid
색상
white
solubility
H2O: >5 mg/mL
저장 온도
2-8°C
SMILES string
Cl.Cl.CN(CCN(C)Cc1cn(-c2cccc(c2)C(F)(F)F)c3ccccc13)CC4=COc5cc(C)c(C)cc5C4=O
InChI
1S/C32H32F3N3O2.2ClH/c1-21-14-28-30(15-22(21)2)40-20-24(31(28)39)18-37(4)13-12-36(3)17-23-19-38(29-11-6-5-10-27(23)29)26-9-7-8-25(16-26)32(33,34)35;;/h5-11,14-16,19-20H,12-13,17-18H2,1-4H3;2*1H
InChI key
GOZMBJCYMQQACI-UHFFFAOYSA-N
유전자 정보
human ... TNF(7124)
mouse ... TNF(21926)
rat ... TNF(24835)
애플리케이션
SPD304 has been used in the inhibition of tumor necrosis factor receptor 1 (TNFR1) in dorsal root ganglion neurons and tumor necrosis factor alpha in colonic epithelial cell lines.
SPD304 may be used in TNF-α-mediated cell signaling studies.
생화학적/생리학적 작용
SPD304 is a small molecule inhibitor of TNF-a activity with a novel mechanism of action. It interferes with protein-protein interactions on the contact surfaces of the trimeric TNF-a subunits, displacing one of the trimer units, resulting in dissociation of the trimer and loss of activity at the receptor TNFR1. SPD304 inhibits TNFR1 receptor binding to TNF-a with an IC50 of 22μM in vitro and inhibits TNF-a-mediated stimulation of IkB degradation in HeLa cells with an IC50 of 4.6 μM.
Trimerization of TNF-α is essential for its biological activity. SPD304 inhibits the trimerization by interacting with Glycine 122 residue. It also inhibits the activity of Receptor activator of nuclear factor-κB ligand (RANKL) by similar interaction.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
개인 보호 장비
dust mask type N95 (US), Eyeshields, Gloves
Dysregulated Up-Frameshift Protein 1 Promotes Ulcerative Colitis Pathogenesis Through the TNFR1-NF-kappaB/MAPKs Pathway
Zhu H, et al.
Digestive Diseases and Sciences, 63(10), 2593-2603 (2018)
Anthi Mettou et al.
SLAS discovery : advancing life sciences R & D, 23(1), 84-93 (2017-06-07)
The aim of this study is to improve the aqueous solubility of a group of compounds without interfering with their bioassay as well as to create a relevant prediction model. A series of 55 potential small-molecule inhibitors of tumor necrosis
Cannabinoid WIN-55,212-2 mesylate inhibits tumor necrosis factor-alpha-induced expression of nitric oxide synthase in dorsal root ganglion neurons
Tan R and Cao L
International Journal of Molecular Medicine, 42(2), 919-925 (2018)
Molly M He et al.
Science (New York, N.Y.), 310(5750), 1022-1025 (2005-11-15)
We have identified a small-molecule inhibitor of tumor necrosis factor alpha (TNF-alpha) that promotes subunit disassembly of this trimeric cytokine family member. The compound inhibits TNF-alpha activity in biochemical and cell-based assays with median inhibitory concentrations of 22 and 4.6
Yang Yu et al.
Hypertension (Dallas, Tex. : 1979), 74(1), 63-72 (2019-06-04)
TNF-α (tumor necrosis factor-α) is initially synthesized as a transmembrane protein that is cleaved by TACE (TNF-α-converting enzyme) to release soluble TNF-α. The elevated level of TNF-α in the brain and circulation in heart failure (HF) suggests an increase in
자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..
고객지원팀으로 연락바랍니다.