Trinitrobenzene sulfonic acid appears as a detonating explosive substance derived from an organic sulfonic acid. Primary hazard is blast of an instantaneous explosion, not flying projectiles or fragments. Under prolonged exposure to fire or heat the containers may explode violently.
溶解度：
In water, 1.58X10+5 mg/L at 25 °C (est)
蒸汽压力：
5.2X10-12 mm Hg at 25 °C (est)
分解：
When heated to decomposition it emits toxic vapors of /nitrogen and sulfur oxides/.
解离常数：
pKa = 0.13
计算性质
辛醇/水分配系数(LogP)：
0.2
重原子数：
19
可旋转键数：
1
环数：
1.0
sp3杂化的碳原子比例：
0.0
拓扑面积：
200
氢给体数：
1
氢受体数：
9
ADMET
毒理性
副作用
Dermatotoxin - 皮肤烧伤。
Dermatotoxin - Skin burns.
来源:Haz-Map, Information on Hazardous Chemicals and Occupational Diseases
The aim of the present study is to investigate the treatment efficiency of intra-rectal (IR) and intra-peritoneal (IP) application of Origanum onites essential oil (OOEO), which is a well-known antioxidant, in the colitis model induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS) and ethanol (E) in comparison with dexamethasone therapy through the morphologic damage score. Monoclonal antibodies against intercellular adhesion molecule-1 (ICAM-1, CD54), anti-rat granulocytes, and myeloperoxidase (MPO), were also investigated immunohistochemically. There was a significant difference in terms of ulceration, mucus cell depletion, inflammatory cell infiltration, vascular dilatation (p<0.001), crypt abscesses (p<0.01), and edema (p<0.05) between OOEO-1mg/kg-IR and control colitis groups. A significant difference was encountered in terms of mucus cell depletion, crypt abscesses, inflammatory cell infiltration, vascular dilatation (p<0.01), and ulceration (p<0.05) between the OOEO-0.1mg/kg-IR and control colitis groups. A significant difference was noticed in terms of ulceration, inflammatory cell infiltration, mucus cell depletion (p<0.001), vascular dilatation (p<0.01), and mucosal atrophy (p<0.05) between the OOEO-1mg/kg-IP and control colitis groups. There was a significant difference in terms of ulceration, mucus cell depletion, inflammatory cell infiltration (p<0.001), crypt abscesses, vascular dilatation (p<0.01), and mucosal atrophy (p<0.05) between the OOEO-0.1mg/kg-IP and control colitis groups. No significant difference was determined in terms of ulceration, inflammatory cyst, mucosal atrophy, edema, and vascular dilatation between the dexamethazone and control colitis groups (p>0.05) ...
A targeted delivery system for inflammatory bowel disease (IBD), Eudragit L100 (EuL)-coated chitosan (Ch)-succinyl-prednisolone (SP) conjugate microspheres (Ch-SP-MS/EuL), was designed and examined in vivo for efficacy and toxicity ... Experimental colitis was induced by instillation of 2,4,6-trinitrobenzenesulfonic acid (TNBS) into the colon in rats. Drugs were administered once or twice a day intragastrically for three consecutive days. Visible colitis severity, colon/body weight ratio and myeloperoxidase activity were measured as inflammatory indices. Toxicity was examined from the decrease in the thymus/body weight ratio. Efficacy was dose-dependent and the greatest in the order Ch-SP-MS/EuL>Ch-SP-MS>prednisolone (PD) alone, and Ch-SP-MS/EuL showed excellent recovery of colitis states. Toxicity was the greatest in the order PD>>Ch-SP-MS>Ch-SP-MS/EuL. Ch-SP-MS and Ch-SP-MS/EuL reduced significantly the thymic atrophy caused by PD. It was demonstrated that Ch-SP-MS/EuL enhanced effectiveness of PD and reduced toxic side effects of PD greatly ...
/The aim of the study was/ to evaluate the protective effects of ilomastat, an exogenous matrix metalloproteinase (MMP) inhibitor, on trinitrobenzenesulfonic acid (TNB)-induced ulcerative colitis (UC) in rats. Male SD rats were randomly divided into model group, protective groups A and B, and normal control group. Rats in the model group received only intra-colonic TNB. Rats in the protective groups A and B received intra-peritoneal ilomastat of 10 mg/kg and 20 mg/kg, respectively, beside TNB. Rats in the normal control group received only intra-colonic normal saline. After 3 wk, segments of colon were obtained. RT-PCR and immunohistochemistry were used to examine the expression of MMP-1 and TIMP-1. Hematoxylin-eosin (HE) staining was used for pathological study. The model of UC was successfully induced in rats. Inflammation of colonic mucosa greatly improved in protective groups A and B. Expression of MMP-1 and TIMP-1 in the model group, protective groups A and B was significantly higher than that in the normal control group (P < 0.0001) with MMP-1 expression increased more significantly than TIMP-1 expression. Expression of MMP-1 in protective groups A and B was significantly lower than that in the model group (P < 0.0001) . Expression of MMP-1 in protective group B was significantly lower than that in protective group A (P < 0.0001). Ilomastat /thus/ improves TNB-induced UC in rats by inhibiting the MMP-1 activity.
... The trinitrobenzenesulfonic acid model of colitis in the rat was used. Rats were treated orally with alendronate and its efficacy compared with that of oral sulfasalazine or vehicle, starting 2 h after colitis induction. The status of the animals was assessed 5 days later ... Alendronate treatment (25 or 75 mg/kg/day) resulted in a decrease in the colonic damage score and loss of body weight (at 25 mg/kg/day only). This was associated to a dramatic reduction in the mRNA levels of interleukin 1 beta (IL-1 beta), monocyte chemoattractant protein 1 (MCP-1) and interleukin 1 receptor antagonist (IL-1 ra). The magnitude of the beneficial effect was comparable to that of sulfasalazine (at a 6-20 fold higher dose) ...
[EN] ISOXAZOLES AS PEPTIDE DEFORMYLASE INHIBITORS<br/>[FR] ISOXAZOLES UTILISES COMME INHIBITEURS DE PEPTIDE DEFORMALYSE
申请人：ARPIDA AS
公开号：WO2005026133A1
公开（公告）日：2005-03-24
Isoxazole compounds of formula (I) and pharmaceutically acceptable salts or esters thereof are peptide deformylase inhibitors useful in the treatment or prevention of infections and other disease in which peptide deformylases are involved, especially in the treatment of bacterial and parasitic infections, for example infections fully or partly caused by microorganisms belonging to Staphylococcus, Enterococcus, Streptococcus, Haemophilus, Moraxella, Escherichia, Mycobacterium, Mycoplasma, Pseudomonas, Chlamydia, Rickettsia, Klebsiella, Shigella, Salmonella, Bordetella, Clostridium, Helicobacter, Campylobacter, Legionella or Neisseria.
[EN] MACROCYCLIZATION OF PEPTIDOMIMETICS<br/>[FR] MACROCYCLISATION DE PEPTIDOMIMÉTIQUES
申请人：UNIV WARWICK
公开号：WO2019186174A1
公开（公告）日：2019-10-03
The invention provides an improved method of macrocyclization of peptidomimetics, as measured by isolated yields and product distribution, which comprises substitution of one or more of the backbone amide C=O bonds with a turn-inducing motif. The method is general with enhancements seen across a range of ring sizes (e.g. tri-, tetra-, penta- and hexapeptides). Specifically, the invention provides a peptidomimetic macrocycle comprising a carbonyl bioisosteric turn-inducing element having the structure: (I) wherein X is a heteroatom; and wherein R1 to R6 are each independently selected from alkyl, aryl, heteroaryl and H.
IMMUNOTHERAPY AGAINST SEVERAL TUMORS, SUCH AS LUNG CANCER, INCLUDING NSCLC
申请人：IMMATICS BIOTECHNOLOGIES GMBH
公开号：US20160168200A1
公开（公告）日：2016-06-16
The present invention relates to peptides, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated cytotoxic T cell (CTL) peptide epitopes, alone or in combination with other tumor-associated peptides that serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses. The present invention relates to more than 70 novel peptide sequences and their variants derived from HLA class I and HLA class II molecules of human tumor cells that can be used in vaccine compositions for eliciting anti-tumor immune responses.
A quencher is disclosed having a compound represented by the following general formula (1):
wherein R
5
each independently represent a halogen atom, an alkyl group, an alkoxy group, an alkylthio group, an amino group having a substituent or not having a substituent, a hydroxy group, an aryl group, an aryloxy group, or an arylalkyl group; R
6
represents a group having a polymerizable unsaturated group, a hydroxy group, or the like; Y
1
represents an oxygen atom, or the like; An
−
represents an anion; Ar
1
represents a specific ring structure; * and ** represent binding positions; Ar
2
represents a benzene ring, a naphthalene ring, or an anthracene ring; n
1
represents a specific integer;
and the following structure (1-10) in the general formula (1) is an asymmetric structure;
(wherein R
5
, Y
1
, Ar
1
, Ar
2
, n
1
, * and ** are the same as described above.).
An object of the present invention is to provide a compound having a modulating activity at an S1P receptor which is useful for preventing and treating autoimmune diseases, allergic diseases, and the like. According to the present invention, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is provided.
