|2-(1H-吲哚-3-基羰基)-4-噻唑羧酸甲酯|CsnPharm

CAS No.: 448906-42-1

Methyl 2-(1H-indole-3-carbonyl)thiazole-4-carboxylate Catalog No. CSN11237

Synonyms: 2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester

ITE is an AhR agonist with Ki value of 3nM, and also inhibits TGF-β-induced human myofibroblast differentiation.

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实验方案

技术信息

生物活性

描述The aryl hydrocarbon receptor (AHR) is a ligand-inducible transcription factor that is best known because it mediates the actions of polycyclic and halogenated aromatic hydrocarbon environmental toxicants such as 3-methylcholanthrene and 2, 3, 7, 8-tetrachlorodibenzo-p-dioxin. ITE is a ligand that binds directly to the AHR to induce receptor activity with K_i of 3 nM ^[3]. Treatment with ITE inhibited the cellular immune responses against the uveitogenic antigen, interphotoreceptor retinoid-binding protein (IRBP), and the CFA component, PPD, as measured in vitro. Treatment with ITE by daily intraperitoneal injection of 0.2 mg efficiently inhibited the development of EAU in B10.A mice induced by immunization with IRBP of 40 μg. Further learning about the effect of ITE treatment on the immune system showed that the proportions of cells expressing IFN-γ or IL-17 were lower in the ITE-treated mice than in their controls ^[4].
临床研究

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NCT00386100	Diabetes Mellitus, Type 2	Phase 4	Completed	-	-
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NCT03108768	Hearing Loss, Bilateral Sensor... more >>ineural, Progressive Collapse <<	Not Applicable	Completed	-	Switzerland ... more >> Sonova AG Stafa, Zürich, Switzerland, 8712 Collapse <<

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参考文献

[1] Wang K, Li Y, et al. An endogenous aryl hydrocarbon receptor ligand inhibits proliferation and migration of human ovarian cancer cells. Cancer Lett. 2013 Oct 28;340(1):63-71.
[2] Song J, Clagett-Dame M, et al. A ligand for the aryl hydrocarbon receptor isolated from lung. Proc Natl Acad Sci U S A. 2002 Nov 12;99(23):14694-9.
[3] Song J, Clagett-Dame M, Peterson RE, Hahn ME, Westler WM, Sicinski RR, DeLuca HF. A ligand for the aryl hydrocarbon receptor isolated from lung. Proc Natl Acad Sci U S A. 2002 Nov 12;99(23):14694-9. doi: 10.1073/pnas.232562899. Epub 2002 Oct 30. PMID: 12409613; PMCID: PMC137481.
[4] Nugent LF, Shi G, Vistica BP, Ogbeifun O, Hinshaw SJ, Gery I. ITE, a novel endogenous nontoxic aryl hydrocarbon receptor ligand, efficiently suppresses EAU and T-cell-mediated immunity. Invest Ophthalmol Vis Sci. 2013 Nov 13;54(12):7463-9. doi: 10.1167/iovs.12-11479. PMID: 24150760; PMCID: PMC3828045.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.4928 mL
- 17.4638 mL
- 34.9277 mL
- 5 mM
- 0.6986 mL
- 3.4928 mL
- 6.9855 mL
- 10 mM
- 0.3493 mL
- 1.7464 mL
- 3.4928 mL

技术信息

CAS号

448906-42-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H10N2O3S

运输

蓝冰

分子量

286.31

别名

2-(1′H-indole-3′-carbonyl)-thiazole-4-carboxylic acid methyl ester

溶解度

DMSO	41.0 mg/mL (143.2 mM)
Water	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00386100	Diabetes Mellitus, Type 2	Phase 4	Completed	-	-
NCT01243424	Diabetes Mellitus, Type 2	Phase 3	Completed	-	-
NCT03108768	Hearing Loss, Bilateral Sensor... more >>ineural, Progressive Collapse <<	Not Applicable	Completed	-	Switzerland ... more >> Sonova AG Stafa, Zürich, Switzerland, 8712 Collapse <<
NCT03569228	Hearing Loss	Not Applicable	Not yet recruiting	October 29, 2022	United States, Tennessee ... more >> Mountain Home VA Medical Center James H. Quillen VA Medical Center, Mountain Home, TN Not yet recruiting Mountain Home, Tennessee, United States, 37684 Contact: Sherri L Smith, PhD 423-926-1171 ext 7569 sherri.smith@va.gov Principal Investigator: Sherri L. Smith, PhD Collapse <<
NCT00386100	-	-	Completed	-	-
NCT02545569	Hearing Loss, Bilateral or Uni... more >>lateral Collapse <<	Not Applicable	Not yet recruiting	December 2020	Switzerland ... more >> Sonova AG Recruiting Staefa, Zürich, Switzerland, 8712 Contact: Jana-Kosima Schwarzlos 0041 58 928 0101 JanaKosima.Schwarzlos@sonova.com Collapse <<
NCT02709486	Osteoarthritis, Hip ... more >> Osteoarthritis, Knee Collapse <<	Phase 3	Active, not recruiting	December 2018	-
NCT01619345	Diabetes Heal... more >>thy Collapse <<	Phase 1	Completed	-	United Kingdom ... more >> Nottingham, United Kingdom, NG11 6JS Collapse <<
NCT02436629	High Intensity Intermittent Sp... more >>orts Performance Collapse <<	Phase 4	Completed	-	Netherlands ... more >> Maastricht University Medical Centre+ Maastricht, Limburg, Netherlands, 6200MD Collapse <<
NCT01746992	ALK-negative Anaplastic Large ... more >>Cell Lymphoma Peripherial T Cell Lymphoma,Not Otherwise Specified Angioimmunoblastic T Cell Lymphoma Enteropathy Associated T Cell Lymphoma Hepatosplenic T Cell Lymphoma Subcutaneous Panniculitis Like T Cell Lymphoma Collapse <<	Phase 4	Active, not recruiting	December 2018	China, Shanghai ... more >> Ruijin hospital Shanghai, Shanghai, China, 200025 Collapse <<
NCT03596346	Food Safety	Not Applicable	Completed	-	Finland ... more >> Satucon Oy/Pihlajalinna Ite Kuopio, Finland, 70100 Collapse <<
NCT03770754	Necrosis	Not Applicable	Enrolling by invitation	January 20, 2019	Mexico ... more >> Jorge Paredes Vieyra Tijuana, Baja California, Mexico, 22000 Jorge Paredes Vieyra Tijuana, Baja Califronia, Mexico, 22000 Jose Clemente Orozco Tijuana, BC, Mexico, 22000 Jose Clemente Tijuana, BC, Mexico, 22000 Collapse <<

Methyl 2-(1H-indole-3-carbonyl)thiazole-4-carboxylate Catalog No. CSN11237

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