RGFP966 (Synonyms: RGFP 966;RGFP-966) |
Catalog No.GC14285
One-Click Copy Product Info
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RGFP966 es un inhibidor de HDAC deN-(o-aminofenil) carboxamida con un IC50 de 0,08 μM para HDAC3,es una clase de inhibidores de unión estrecha competitivos de encendido/apagado lento dirigidos a HDAC3.
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Cas No.: 1357389-11-7
Sample solution is provided at 25 µL, 10mM.
RGFP966 es un inhibidor de HDAC deN-(o-aminofenil) carboxamida con un IC50 de 0,08 μM para HDAC3,es una clase de inhibidores de unión estrecha competitivos de encendido/apagado lento dirigidos a HDAC3.RGFP966 ha demostrado suprimir las respuestasinflamatorias en las diversas enfermedades inflamatorias[1-3].
RGFP966(1μM ;20 h) atenúa la expresión génica inflamatoria en macrófagos RAW 264.7 estimulados por LPS/IFNγ[3].
RGFP966(10-25μM;48h) inhibió tanto la proliferacióncomo la migración de las células de HCC[4].
RGFP966(10 mg/kg;6h before SBI) inhibió la regulación positiva de HDAC3 y salvó las células nerviosas alrededor del área dañada en ratas con lesión cerebral quirúrgica(SBI)[5]. RGFP966(10 mg/kg/día;i.p; 5días)podría mejorar los comportamientos depresivos inducidos por LPS en los ratones.RGFP966 tratamiento reguló a la baja los niveles de expresión del receptor tipo 4 (TLR4),el receptor similiar al dominio de oligomerización de unión a nucleótidos que contiene el dominio pirina-3(NLRP3),la caspasa-1 y la interleucina-1β (IL-1β) [6]. RGFP966(10 mg/kg or 20 mg/kg) reducen la expresión de HDAC3 y las actividades de HDAC3,y luego disminuyen el reclutamineto de eosinó´filos y mastocitos,la proliferación de las células caliciformes y los niveles de citoquinas inflamatorias,loque resulta en elalivio de las respuestas alérgicas e inflamatorias en los ratones con rinitis alérgica(AR)[7].
References:
[1]. Malvaez M, McQuown SC, et,al. HDAC3-selective inhibitor enhances extinction of cocaine-seeking behavior in a persistent manner. Proc Natl Acad Sci U S A. 2013 Feb 12;110(7):2647-52. doi: 10.1073/pnas.1213364110. Epub 2013 Jan 7. PMID: 23297220; PMCID: PMC3574934.
[2]. Chou CJ, Herman D, et,al. Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I histone deacetylases. J Biol Chem. 2008 Dec 19;283(51):35402-9. doi: 10.1074/jbc.M807045200. Epub 2008 Oct 24. PMID: 18953021; PMCID: PMC2602898.
[3]. Leus NG, van der Wouden PE, et,al. HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity. Biochem Pharmacol. 2016 May 15;108:58-74. doi: 10.1016/j.bcp.2016.03.010. Epub 2016 Mar 16. PMID: 26993378; PMCID: PMC4844503.
[4]. Yu X, Yang F, et,al. RGFP966 Suppresses Tumor Growth and Migration Through Inhibition of EGFR Expression in Hepatocellular Carcinoma Cells in vitro. Drug Des Devel Ther. 2020 Jan 10;14:121-128. doi: 10.2147/DDDT.S234871. PMID: 32021097; PMCID: PMC6959505.
[5]. Gu HP, Wu XF, et,al. RGFP966 exerts neuroprotective effect via HDAC3/Nrf2 pathway after surgical brain injury in rats. Heliyon. 2023 Jul 12;9(7):e18160. doi: 10.1016/j.heliyon.2023.e18160. PMID: 37539293; PMCID: PMC10395478.
[6]. Bian HT, Xiao L, et,al. RGFP966 is protective against lipopolysaccharide-induced depressive-like behaviors in mice by inhibiting neuroinflammation and microglial activation. Int Immunopharmacol. 2021 Dec;101(Pt B):108259. doi: 10.1016/j.intimp.2021.108259. Epub 2021 Oct 16. PMID: 34666303.
[7]. Zhang W, Sun X, et,al. RGFP966, a selective HDAC3 inhibitor, ameliorates allergic and inflammatory responses in an OVA-induced allergic rhinitis mouse model. Int Immunopharmacol. 2021 Apr;93:107400. doi: 10.1016/j.intimp.2021.107400. Epub 2021 Jan 30. PMID: 33529911.
| Experimentos celulares [1]: | |
Líneas celulares | Macrophago Ratón RAW 264.7 |
Método de preparación | Las células se incubaron con RGFP966 de 1μM durante 20 h y se estimularon con LPS/IFNγ durante las últimas 4 h. |
Condiciones de reacción | 1μM ;20 h |
Aplicación | RGFP966 atenúa la expresión génica inflamatoria en macrófagos RAW 264.7 estimulados por LPS/IFNγ. |
| Experimentos con animales [2]: | |
Modelos animales | Los ratones machos adultos C57BL/6J (peso 20–22g) |
Método de preparación | Los ratones se dividieron en cuatro grupos: control groupo, LPS groupo, LPS + RGFP966 groupo, y RGFP966 groupo. LPS se solubilizó en la solución salina tamponada con fosfato(PBS) y se inyectó por vía intraperitoneal (i.p.) a una dosis en dimetilsulfóxido(DMSO),PEG300 y la solución salina,y luego se inyectó i.p.a una dosis de 10 mg/kg/día para un total de cinco inyecciones. |
Forma de dosificación | 10 mg/kg/día;i.p; 5dÍas |
Aplicación | RGFP966 tratamiento revirtió los cambios de peso corporal inducidaos por LPS en los ratones. |
References: [1]. Leus NG, van der Wouden PE, et,al. HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-?B p65 transcriptional activity. Biochem Pharmacol. 2016 May 15;108:58-74. doi: 10.1016/j.bcp.2016.03.010. Epub 2016 Mar 16. PMID: 26993378; PMCID: PMC4844503. [2]. Bian HT, Xiao L, et,al. RGFP966 is protective against lipopolysaccharide-induced depressive-like behaviors in mice by inhibiting neuroinflammation and microglial activation. Int Immunopharmacol. 2021 Dec;101(Pt B):108259. doi: 10.1016/j.intimp.2021.108259. Epub 2021 Oct 16. PMID: 34666303. | |
| Cas No. | 1357389-11-7 | SDF | |
| Sinónimos | RGFP 966;RGFP-966 | ||
| Canonical SMILES | C1=CC=C(C=C1)C=CCN2C=C(C=N2)C=CC(=O)NC3=C(C=C(C=C3)F)N | ||
| Formula | C21H19FN4O | M.Wt | 362.4 |
| Solubility | ≥ 18.12mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7594 mL | 13.7969 mL | 27.5938 mL |
| 5 mM | 551.9 μL | 2.7594 mL | 5.5188 mL |
| 10 mM | 275.9 μL | 1.3797 mL | 2.7594 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)