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MedChemExpress - Model Penfluridol - ...

MedChemExpress - Model Penfluridol - 26864-56-2

Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml[1][2][3][4].

Penfluridol

MCE China：Penfluridol

Brand：MedChemExpress (MCE)

Cat. No.HY-B1077

CAS：26864-56-2

Synonyms：R-16341

Purity：99.84%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml.

In Vitro：Penfluridol (R-16341; 1.25-40 μM; 24, 48 h) reduces cell viability of human AML cells harboring FLT3-WT or the FLT3-ITD mutation[2]. Penfluridol (7.5 μM; 24 h) results in the apoptosis of AML cells harboring FLT3-WT and FLT3-ITD mutation[2]. Penfluridol (1.25-7.5 μM; 24 h) induces ROS-mediated autophagy via triggering LC3 turnover and acidic vesicular organelle (AVO) formation[2]. Penfluridol (1 μM; for 2 h) obviously inhibits TNFα-induced phosphorylation levels of ERK, JNK, and p38[3]. Penfluridol (1 μM; for 2 h) inhibits TNFα-induced mRNA expressions of IL-1β, IL-6, IL-17, and NOS2[3]. Penfluridol suppresses the differentiation of spleen naive CD4+T cells to TH1 and TH17 and inhibits M1 macrophage polarization[3].

In Vivo：Penfluridol (10 mg/kg; daily oral gavage; from the 18th day after the first immunization) significantly reduced severity of collagen-induced arthritis[3].

IC50 & Target：D2 Receptor

References：

[1]. Eyal Zur, et al. Penfluridol, a Unique Psychiatric Medicine for the Treatment of Chronic Schizophrenia. Int J Pharm Compd. 2019 Mar-Apr;23(2):113-119. [Content Brief]

[2]. Szu-Yuan Wu, et al. Penfluridol triggers cytoprotective autophagy and cellular apoptosis through ROS induction and activation of the PP2A-modulated MAPK pathway in acute myeloid leukemia with different FLT3 statuses. J Biomed Sci. 2019 Aug 31;26(1):63. [Content Brief]

[3]. Yue-Hong Chen, et al. Penfluridol targets acid sphingomyelinase to inhibit TNF signaling and is therapeutic against inflammatory autoimmune diseases. Arthritis Res Ther. 2022 Jan 19;24(1):27. [Content Brief]

[4]. Xianghai Zeng, et al. Drug repurposing: Antimicrobial and antibiofilm effects of penfluridol against Enterococcus faecalis. Microbiologyopen. 2021 Jan;10(1):e1148. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   It has a professional experimental center and strict quality control and verification system；
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•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。