R-7050 | CAS#303997-35-5 | TNF-α receptor antagonist

MedKoo Cat#: 562551 | Name: R-7050

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

R-7050 is a TNF-α receptor antagonist. It acts by blocking receptor-adaptor molecule complex formation and subsequent receptor internalization, but not TNF-α ligand-receptor binding.

Chemical Structure

R-7050

CAS#303997-35-5

Theoretical Analysis

MedKoo Cat#: 562551

Name: R-7050

CAS#: 303997-35-5

Chemical Formula: C16H8ClF3N4S

Exact Mass: 380.0110

Molecular Weight: 380.77

Elemental Analysis: C, 50.47; H, 2.12; Cl, 9.31; F, 14.97; N, 14.71; S, 8.42

Price and Availability

Size	Price	Availability
1mg	USD 250.00	2 weeks
5mg	USD 450.00	2 weeks
10mg	USD 700.00	2 weeks

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Synonym

R-7050; R 7050; R7050; TNF-α Antagonist III;

IUPAC/Chemical Name

8-Chloro-4-(phenylthio)-1-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]quinoxaline

InChi Key

SUUMKHOVGVYGOP-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H8ClF3N4S/c17-9-6-7-11-12(8-9)24-13(22-23-15(24)16(18,19)20)14(21-11)25-10-4-2-1-3-5-10/h1-8H

SMILES Code

FC(C1=NN=C2N1C3=C(C=CC(Cl)=C3)N=C2SC4=CC=CC=C4)(F)F

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO (need ultrasonic)

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

R-7050 acts by blocking receptor-adaptor molecule complex formation and subsequent receptor internalization, but not TNF-α ligand-receptor binding.

In vitro activity:

To be determined

In vivo activity:

This study found that repetitive injection of Taraxaci Herba and/or R-7050 reduced the symptoms of Behçet's disease and significantly decreased IL-6, IL-1β, and TNFα in blood sera of mice. This treatment reduced the ulcers and the deterioration of skin. Reference: Integr Med Res. 2021 Sep;10(3):100720. https://pubmed.ncbi.nlm.nih.gov/33898245/

	Solvent	mg/mL	mM
Solubility
	DMSO (need ultrasonic)	25.0	65.66

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 380.77 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Cha M, Kwon M, Park M, Oh JH, Sung KK, Lee BH. Combined treatment of Taraxaci Herba and R7050 alleviates the symptoms of herpes simplex virus-induced Behçet's disease in rats. Integr Med Res. 2021 Sep;10(3):100720. doi: 10.1016/j.imr.2021.100720. Epub 2021 Feb 17. PMID: 33898245; PMCID: PMC8059053. 2. Wen Y, Lu X, Ren J, Privratsky JR, Yang B, Rudemiller NP, Zhang J, Griffiths R, Jain MK, Nedospasov SA, Liu BC, Crowley SD. KLF4 in Macrophages Attenuates TNFα-Mediated Kidney Injury and Fibrosis. J Am Soc Nephrol. 2019 Oct;30(10):1925-1938. doi: 10.1681/ASN.2019020111. Epub 2019 Jul 23. PMID: 31337692; PMCID: PMC6779357.

In vitro protocol:

To be determined

In vivo protocol:

1: Li K, Ling H, Huang W, Luo W, Gu C, Tao B, Xie Q, Qiu P. Single-cell RNA- sequencing analysis reveals α-syn induced astrocyte-neuron crosstalk-mediated neurotoxicity. Int Immunopharmacol. 2024 Sep 30;139:112676. doi: 10.1016/j.intimp.2024.112676. Epub 2024 Jul 24. PMID: 39053230. 2: Amititeloaie C, Chelaru L, Geleţu GL, Sava A, Jităreanu A, Tibeică AM, Costuleanu M. Apoptosis of pro-B lymphocytes induced by NR4A1 activation in the presence of gingival fibroblast exosomes and TNFα, caspase 8, STAT3, and Akt pathways modulators. Rom J Morphol Embryol. 2023 Jan-Mar;64(1):35-40. doi: 10.47162/RJME.64.1.04. PMID: 37128789; PMCID: PMC10257780. 3: Ji M, Sun Q, Zhang G, Huang Z, Zhang Y, Shen Q, Guan H. Microglia-derived TNF-α mediates Müller cell activation by activating the TNFR1-NF-κB pathway. Exp Eye Res. 2022 Jan;214:108852. doi: 10.1016/j.exer.2021.108852. Epub 2021 Nov 18. PMID: 34801535. 4: Lin SY, Wang YY, Chang CY, Wu CC, Chen WY, Liao SL, Chen CJ. TNF-α Receptor Inhibitor Alleviates Metabolic and Inflammatory Changes in a Rat Model of Ischemic Stroke. Antioxidants (Basel). 2021 May 26;10(6):851. doi: 10.3390/antiox10060851. PMID: 34073455; PMCID: PMC8228519. 5: Pal A, Tapadar P, Pal R. Exploring the Molecular Mechanism of Cinnamic Acid- Mediated Cytotoxicity in Triple Negative MDA-MB-231 Breast Cancer Cells. Anticancer Agents Med Chem. 2021;21(9):1141-1150. doi: 10.2174/1871520620666200807222248. PMID: 32767960. 6: Liu J, Que K, Liu Y, Zang C, Wen J. Tumor Necrosis Factor-α Regulates the TRPA1 Expression in Human Odontoblast-Like Cells. J Pain Res. 2020 Jul 6;13:1655-1664. doi: 10.2147/JPR.S255288. PMID: 32753941; PMCID: PMC7352379. 7: Ayo TE, Adhikari P, Sugita S, Xu H. TNF Production in Activated RBL-2H3 Cells Requires Munc13-4. Inflammation. 2020 Apr;43(2):744-751. doi: 10.1007/s10753-019-01161-4. PMID: 31897916; PMCID: PMC7176528. 8: Ding L, Kang Y, Dai HB, Wang FZ, Zhou H, Gao Q, Xiong XQ, Zhang F, Song TR, Yuan Y, Liu M, Zhu GQ, Zhou YB. Adipose afferent reflex is enhanced by TNFα in paraventricular nucleus through NADPH oxidase-dependent ROS generation in obesity-related hypertensive rats. J Transl Med. 2019 Aug 7;17(1):256. doi: 10.1186/s12967-019-2006-0. PMID: 31391086; PMCID: PMC6686415. 9: Wen Y, Lu X, Ren J, Privratsky JR, Yang B, Rudemiller NP, Zhang J, Griffiths R, Jain MK, Nedospasov SA, Liu BC, Crowley SD. KLF4 in Macrophages Attenuates TNFα-Mediated Kidney Injury and Fibrosis. J Am Soc Nephrol. 2019 Oct;30(10):1925-1938. doi: 10.1681/ASN.2019020111. Epub 2019 Jul 23. PMID: 31337692; PMCID: PMC6779357. 10: Naime ACA, Bonfitto PHL, Solon C, Lopes-Pires ME, Anhê GF, Antunes E, Marcondes S. Tumor necrosis factor alpha has a crucial role in increased reactive oxygen species production in platelets of mice injected with lipopolysaccharide. Platelets. 2019;30(8):1047-1052. doi: 10.1080/09537104.2019.1588241. Epub 2019 May 10. PMID: 31076004. 11: Zhong B, Ma S, Wang DH. Ablation of TRPV1 Elevates Nocturnal Blood Pressure in Western Diet-fed Mice. Curr Hypertens Rev. 2019;15(2):144-153. doi: 10.2174/1573402114666181031141840. PMID: 30381083; PMCID: PMC6635649. 12: Mulay SR, Eberhard JN, Desai J, Marschner JA, Kumar SV, Weidenbusch M, Grigorescu M, Lech M, Eltrich N, Müller L, Hans W, Hrabě de Angelis M, Vielhauer V, Hoppe B, Asplin J, Burzlaff N, Herrmann M, Evan A, Anders HJ. Hyperoxaluria Requires TNF Receptors to Initiate Crystal Adhesion and Kidney Stone Disease. J Am Soc Nephrol. 2017 Mar;28(3):761-768. doi: 10.1681/ASN.2016040486. Epub 2016 Sep 9. PMID: 27612997; PMCID: PMC5328164. 13: Yang N, Liang Y, Yang P, Wang W, Zhang X, Wang J. TNF-α receptor antagonist attenuates isoflurane-induced cognitive impairment in aged rats. Exp Ther Med. 2016 Jul;12(1):463-468. doi: 10.3892/etm.2016.3262. Epub 2016 Apr 18. PMID: 27347079; PMCID: PMC4906939. 14: Ma Y, Cheng Q, Wang E, Li L, Zhang X. Inhibiting tumor necrosis factor-α signaling attenuates postoperative cognitive dysfunction in aged rats. Mol Med Rep. 2015 Aug;12(2):3095-100. doi: 10.3892/mmr.2015.3744. Epub 2015 May 7. PMID: 25955232. 15: Wu W, Zhang H. Role of tumor necrosis factor-α and interleukin-1β in anorexia induction following oral exposure to the trichothecene deoxynivalenol (vomitoxin) in the mouse. J Toxicol Sci. 2014;39(6):875-86. doi: 10.2131/jts.39.875. PMID: 25392278. 16: King MD, Alleyne CH Jr, Dhandapani KM. TNF-alpha receptor antagonist, R-7050, improves neurological outcomes following intracerebral hemorrhage in mice. Neurosci Lett. 2013 May 10;542:92-6. doi: 10.1016/j.neulet.2013.02.051. Epub 2013 Mar 7. PMID: 23499961; PMCID: PMC3744337.