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| | 1H-Indol-7-amine, 5-[(1,1-dioxido-4-thiomorpholinyl)methyl]-2-phenyl-N-(tetrahydro-2H-pyran-4-yl)- Basic information |
| | 1H-Indol-7-amine, 5-[(1,1-dioxido-4-thiomorpholinyl)methyl]-2-phenyl-N-(tetrahydro-2H-pyran-4-yl)- Chemical Properties |
| Boiling point | 736.2±60.0 °C(Predicted) | | density | 1.319±0.06 g/cm3(Predicted) | | solubility | Acetonitrile: Slightly soluble: 0.1-1 mg/ml
DMSO: Sparingly soluble: 1-10 mg/ml | | form | Solid | | pka | 17.48±0.30(Predicted) | | color | Off-white to yellow | | Cosmetics Ingredients Functions | ANTIOXIDANT
SKIN PROTECTING |
| | 1H-Indol-7-amine, 5-[(1,1-dioxido-4-thiomorpholinyl)methyl]-2-phenyl-N-(tetrahydro-2H-pyran-4-yl)- Usage And Synthesis |
| Uses | NecroX-7 is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor. NecroX-7 can be used as an antidote to acetaminophen toxicity. NecroX-7 exerts a protective effect by preventing the release of HMGB1 in ischemia/reperfusion injury. NecroX-7 inhibits the HMGB1-induced release of TNF and IL-6, as well as the expression of TLR-4 and receptor for advanced glycation end products. NecroX-7 can be used graft-versus-host disease (GVHD) research[1]. | | in vivo | NecroX-7 (0-0.3 mg/kg, IV, once injection at 2-d intervals, for 2 weeks) significantly attenuates GVHD-related mortality and inhibits severe tissue damage[1].
NecroX-7 protects mice against lethal GVHD by reciprocal regulation of regulatory T/Th1 cells, attenuating systemic HMGB1 accumulation and inhibiting HMGB1-mediated inflammatory response[1]. | Animal Model: | Female BALB/c and C57BL/6 mice (Eight-week-old, with GVHD)[1] | | Dosage: | 0.03, 0.1, and 0.3 mg/kg | | Administration: | IV, once injection at 2-d intervals, for 2 weeks | | Result: | Observed statistically significant prolonged survival at doses ≥0.1 mg/kg: 30–60% of mice in these treatment groups survived for >50 d. Significantly improved clinical signs and prolonged survival, and the mice showed a reduction in clinical manifestations of acute GVHD, including weight loss, hunched posture, diarrhea, and ruffled fur. |
| | IC 50 | IL-6; TLR4 | | References | [1] Im KI, et al. The Free Radical Scavenger NecroX-7 Attenuates Acute Graft-versus-Host Disease via Reciprocal Regulation of Th1/Regulatory T Cells and Inhibition of HMGB1 Release. J Immunol. 2015 Jun 1;194(11):5223-32. DOI:10.4049/jimmunol.1402609
[2] JI-HOON PARK. An indole derivative protects against acetaminophen-induced liver injury by directly binding to N-acetyl-p-benzoquinone imine in mice.[J]. Antioxidants & redox signaling, 2013, 18 14: 1713-1722. DOI: 10.1089/ars.2012.4677
[3] JOONGHOON PARK . NecroX-7 prevents oxidative stress-induced cardiomyopathy by inhibition of NADPH oxidase activity in rats[J]. Toxicology and applied pharmacology, 2012, 263 1: Pages 1-6. DOI: 10.1016/j.taap.2012.05.014
[4] YANG LU, JINXIN CHE* Discovery of New Phenyltetrazolium Derivatives as Ferroptosis Inhibitors for Treating Ischemic Stroke: An Example Development from Free Radical Scavengers[J]. Journal of Medicinal Chemistry, 2024, 67 14: 11712-11731 11712-11731. DOI: 10.1021/acs.jmedchem.4c0021110.1021/acs.jmedchem.4c00211 |
| | 1H-Indol-7-amine, 5-[(1,1-dioxido-4-thiomorpholinyl)methyl]-2-phenyl-N-(tetrahydro-2H-pyran-4-yl)- Preparation Products And Raw materials |
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