R-7050
Based on 29 publication(s) in Google Scholar
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
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- 純度: 99.96%
- CAS 番号: 303997-35-5
- 分子式: C16H8ClF3N4S
- 分子量:380.77
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 R-7050
More- Cell Death Differ. 2021 Sep;28(9):2728-2744. [Abstract]
- Acta Pharm Sin B. 2024 Oct;14(10):4544-4559. [Abstract]
- J Control Release. 2025 Jan 13:379:266-284. [Abstract]
- J Neuroinflammation. 2023 Jun 1;20(1):137. [Abstract]
- J Neuroinflammation. 2019 Nov 26;16(1):234. [Abstract]
- Cell Death Dis. 2025 Feb 25;16(1):129. [Abstract]
- NPJ Biofilms Microbiomes. 2024 Dec 19;10(1):154. [Abstract]
- Phytomedicine. 2024 Jul 25:130:155482. [Abstract]
- Free Radic Biol Med. 2023 Feb 1:195:329-342. [Abstract]
- J Transl Med. 2021 Dec 7;19(1):497. [Abstract]
- Cell Rep. 2024 Jul 9;43(7):114453. [Abstract]
- Cell Rep. 2022 Jul 5;40(1):111033. [Abstract]
- Neural Regen Res. 2026 Jan 1;21(1):346-356. [Abstract]
- Ecotoxicol Environ Saf. 2025 Dec 2:308:119482. [Abstract]
- Antioxid Redox Signal. 2023 Apr;38(10-12):747-767. [Abstract]
- Ecotoxicol Environ Saf. 2022 May 1;236:113468. [Abstract]
- J Invest Dermatol. 2022 Nov;142(11):3041-3051.e10. [Abstract]
- Inflamm Res. 2025 Feb 19;74(1):42. [Abstract]
- Int Immunopharmacol. 2025 Apr 4:154:114574. [Abstract]
- Int Immunopharmacol. 2025 Feb 3:149:114192. [Abstract]
- Mol Neurobiol. 2025 Jul;62(7):8298-8312. [Abstract]
- J Cell Mol Med. 2020 Sep;24(18):10604-10614. [Abstract]
- J Inflamm Res. 2025 Feb 19:18:2447-2464. [Abstract]
- Sci Rep. 2025 May 12;15(1):16448. [Abstract]
- J Photochem Photobiol B. 2026 May:278:113433. [Abstract]
- J Immunol. 2022 Nov 1;209(9):1796-1805. [Abstract]
- Mol Immunol. 2021 Feb;130:85-95. [Abstract]
- Asian J Androl. 2022 Sep-Oct;24(5):513-520. [Abstract]
- bioRxiv. 2025 Sep 12.
生物活性
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CD40 |
R-7050 (TNF-α Antagonist III) is a potent and fully reversible hit with greater selectivity toward TNFα. In TNFα-induced? intercellular adhesion molecule 1 (ICAM-1)? expression, R-7050 inhibition potency (EC50=0.63 μM) is 2- to 3-fold greater than EC50 for IL-1β-induced ICAM-1 expression (EC50=1.45 2 μM). R-7050 inhibits phosphorylation of both the JNK pathway (MKK4, JNKs, and ATF2) and p38 pathway (MKK3/6, p38, and MAPKAP2)[1].
R-7050 is a cell-permeable triazoloquinoxaline compound that selectively inhibits TNF-α induced cellular signaling. Unlike biologic TNF inhibitors (e.g. Infliximab, Etanercept, Adalimumab) that directly bind TNF-α and function as decoy receptors, R-7050 does not affect binding of TNF-α to TNFR. In contrast, R-7050 selectively inhibits the association of TNFR with intracellular adaptor molecules (e.g. TRADD, RIP), limits receptor internalization, and prevents subsequent cellular responses after TNF-α binding[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 303997-35-5
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性状 Solid
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分子量 380.77
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分子式 C16H8ClF3N4S
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Color Light yellow to yellow
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SMILES
FC(F)(C1=NN=C2N1C3=CC(Cl)=CC=C3N=C2SC4=CC=CC=C4)F
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別名
TNF-α Antagonist III
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (29)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
PP2Acα promotes macrophage accumulation and activation to exacerbate tubular cell death and kidney fibrosis through activating Rap1 and TNFα production. [Abstract]2021 Sep;28(9):2728-2744. PMID: 33934104 -
Acta Pharm Sin B
Choroid plexus CCL2‒CCR2 signaling orchestrates macrophage recruitment and cerebrospinal fluid hypersecretion in hydrocephalus. [Abstract]2024 Oct;14(10):4544-4559. PMID: 39525574 -
J Control Release
Ropivacaine and celecoxib-loaded injectable composite hydrogel for improved chronic pain-exacerbated myocardial ischemia-reperfusion injury. [Abstract]2025 Jan 13:379:266-284. PMID: 39800238 -
J Neuroinflammation
Microglia-derived TNF-α contributes to RVLM neuronal mitochondrial dysfunction via blocking the AMPK-Sirt3 pathway in stress-induced hypertension. [Abstract]2023 Jun 1;20(1):137. PMID: 37264405 -
J Neuroinflammation
The role of Toll-like receptor 4 in apoptosis of brain tissue after induction of intracerebral hemorrhage. [Abstract]2019 Nov 26;16(1):234. PMID: 31771613 -
Cell Death Dis
Tumor vascular endothelial cells promote immune escape by upregulating PD-L1 expression via crosstalk between NF-κB and STAT3 signaling pathways in nasopharyngeal carcinoma. [Abstract]2025 Feb 25;16(1):129. PMID: 40000620 -
NPJ Biofilms Microbiomes
Roles of gut microbiome-associated metabolites in pulmonary fibrosis by integrated analysis. [Abstract]2024 Dec 19;10(1):154. PMID: 39702426 -
Phytomedicine
Ophiopogonin D alleviates acute lung injury by regulating inflammation via the STAT3/A20/ASK1 axis. [Abstract]2024 Jul 25:130:155482. PMID: 38824823 -
Free Radic Biol Med
2023 Feb 1:195:329-342. PMID: 36610561 -
J Transl Med
Delineation of colorectal cancer ligand-receptor interactions and their roles in the tumor microenvironment and prognosis. [Abstract]2021 Dec 7;19(1):497. PMID: 34876143 -
Cell Rep
Extracellular vesicles from alveolar macrophages harboring phagocytosed methicillin-resistant Staphylococcus aureus induce necroptosis. [Abstract]2024 Jul 9;43(7):114453. PMID: 38985677 -
Cell Rep
Bacteria reduce flagellin synthesis to evade microglia-astrocyte-driven immunity in the brain. [Abstract]2022 Jul 5;40(1):111033. PMID: 35793624 -
Neural Regen Res
2026 Jan 1;21(1):346-356. PMID: 39927762 -
Ecotoxicol Environ Saf
Asiaticoside ameliorates pyrimethanil-induced autophagy-dependent liver injury by suppressing CRHR1. [Abstract]2025 Dec 2:308:119482. PMID: 41338089 -
Antioxid Redox Signal
Radiation-induced bystander effect on the genome of bone marrow mesenchymal stem cells in lung cancer. [Abstract]2023 Apr;38(10-12):747-767. PMID: 36242096 -
Ecotoxicol Environ Saf
2022 May 1;236:113468. PMID: 35378400 -
J Invest Dermatol
M1 Macrophages Induce Protumor Inflammation in Melanoma Cells through TNFR-NF-κB Signaling. [Abstract]2022 Nov;142(11):3041-3051.e10. PMID: 35580697 -
Inflamm Res
Exploring macrophage and nerve interaction in endometriosis-associated pain: the inductive role of IL-33. [Abstract]2025 Feb 19;74(1):42. PMID: 39969583 -
Int Immunopharmacol
Low-frequency ultrasound alleviates pulmonary inflammation induced by Klebsiella pneumoniae in mice by inhibiting the TNFR1/NF-κB pathway. [Abstract]2025 Apr 4:154:114574. PMID: 40188523 -
Int Immunopharmacol
Inhibiting HMGB1/AGER/NF-κB pathway prevents pro-inflammatory microglia polarization and protect photoreceptors in retinitis pigmentosa. [Abstract]2025 Feb 3:149:114192. PMID: 39904032 -
Mol Neurobiol
TNF-α Enhanced Activity of Sympathetic Neurons in Superior Cervical Ganglion to Promote Chronic Sleep Deprivation-Related Hyperalgesia. [Abstract]2025 Jul;62(7):8298-8312. PMID: 39992586 -
J Cell Mol Med
PDX regulates inflammatory cell infiltration via resident macrophage in LPS-induced lung injury. [Abstract]2020 Sep;24(18):10604-10614. PMID: 32735065 -
J Inflamm Res
Cigarette Smoking Induces Skeletal Muscle Atrophy in Mice by Activated Macrophage-Mediated Pyroptosis. [Abstract]2025 Feb 19:18:2447-2464. PMID: 39991657 -
Sci Rep
TNF-α inhibits Epstein Barr virus reactivation through the GPX4 mediated glutathione pathway. [Abstract]2025 May 12;15(1):16448. PMID: 40355596 -
J Photochem Photobiol B
Targeting TNF-SDH axis in macrophages reverses abnormal succinate metabolism and M1 polarization to alleviate UVB-induced skin damage. [Abstract]2026 May:278:113433. PMID: 41921367 -
J Immunol
RNF186/EPHB2 Axis Is Essential in Regulating TNF Signaling for Colorectal Tumorigenesis in Colorectal Epithelial Cells. [Abstract]2022 Nov 1;209(9):1796-1805. PMID: 36130827 -
Mol Immunol
Impact of knockdown LincRNA-Cox2 on apoptosis of macrophage infected with Bacillus Calmette-Guérin. [Abstract]2021 Feb;130:85-95. PMID: 33250268 -
Asian J Androl
Combined treatment with dihydrotestosterone and lipopolysaccharide modulates prostate homeostasis by upregulating TNF-α from M1 macrophages and promotes proliferation of prostate stromal cells. [Abstract]2022 Sep-Oct;24(5):513-520. PMID: 34975070 -
溶剤 & 溶解度
DMSO : 25 mg/mL (65.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.57 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
Mice[2]
A mouse collagenase model of ICH is utilized. Briefly, male CD-1 mice (8-10 weeks old) are placed into a stereotactic frame and a 0.5 mm diameter burr hole is drilled over the parietal cortex, 2.2 mm lateral to the bregma. A 26-gauge Hamilton syringe, loaded with 0.04 U of bacterial type IV collagenase in 0.5 μL saline, is lowered 3 mm deep from the skull surface directly into the left striatum. The syringe is depressed at a rate of 450 nL/min and left in place for several minutes after the procedure to prevent solution reflux and excess diffusion. Sham animals undergo the same surgical procedure, except that saline is stereotactically injected rather than collagenase. After the syringe is removed, bone wax is used to close the burr hole, the incision is surgically stapled, and mice are kept warm until recovery of the righting reflex. R-7050 (6-18 mg/kg) is administered via intraperitoneal route at the time of injury or up to 2 h post-ICH[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Gururaja TL, et al. A class of small molecules that inhibit TNFalpha-induced survival and death pathways viaprevention of interactions between TNFalphaRI, TRADD, and RIP1. Chem Biol. 2007 Oct;14(10):1105-18. [Content Brief]
[2]. King MD, et al. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebralhemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6263 mL | 13.1313 mL | 26.2626 mL | 65.6564 mL |
| 5 mM | 0.5253 mL | 2.6263 mL | 5.2525 mL | 13.1313 mL | |
| 10 mM | 0.2626 mL | 1.3131 mL | 2.6263 mL | 6.5656 mL | |
| 15 mM | 0.1751 mL | 0.8754 mL | 1.7508 mL | 4.3771 mL | |
| 20 mM | 0.1313 mL | 0.6566 mL | 1.3131 mL | 3.2828 mL | |
| 25 mM | 0.1051 mL | 0.5253 mL | 1.0505 mL | 2.6263 mL | |
| 30 mM | 0.0875 mL | 0.4377 mL | 0.8754 mL | 2.1885 mL | |
| 40 mM | 0.0657 mL | 0.3283 mL | 0.6566 mL | 1.6414 mL | |
| 50 mM | 0.0525 mL | 0.2626 mL | 0.5253 mL | 1.3131 mL | |
| 60 mM | 0.0438 mL | 0.2189 mL | 0.4377 mL | 1.0943 mL |
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