Trifluoperazine 2HCl

製品コードS3201 バッチS320101

印刷

化学情報

Chemical Structure Synonyms SKF5019 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H24F3N3S.2HCl
分子量 480.42 CAS No. 440-17-5
Solubility (25°C)* 体外 Water 96 mg/mL (199.82 mM)
Ethanol 96 mg/mL (199.82 mM)
DMSO 88 mg/mL (183.17 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Trifluoperazine (NSC-17474, RP-7623, SKF-5019) 2HCl is a dopamine D2 receptor inhibitor with IC50 of 1.1 nM. Trifluoperazine also inhibits calmodulin (CaM).
in vitro Trifluoperazine binds to α1A- and α1B-adrenoceptor with Ki value of 27.6 nM and 19.2 nM, respectively, with α1B/α1A ratio of 0.7. [2] Trifluoperazine inhibits Mycobacterium tuberculosis (Mtb) with MICs of 7.6 μg/mL. [3] Trifluoperazine (< 14.78 mM) suppresses the activities of the mouse splenic NK cell cytotoxicity and the effector-target cell conjugation in a dose dependent manner. Trifluoperazine suppresses interferon-alpha or interleukin-2 induced augmentation of the cytolytic activity of NK cells. [4] Trifluoperazine inhibits the gene expression of voltage-dependent potassium channel Kv2.1 from human brain (hKv2.1). [5]
in vivo Trifluoperazine dose dependently decreases avoidance responses and increases response failures in rats where behavior is maintained under a discrete-trial avoidance. [6]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
Receptor binding studies are conducted using membranes from the cloned dopamine D2 receptor. For both receptors the ligand used is [3H]YM-09151-2 (specific activity 86.1 Ci/mmol). Incubation is for 1 hour at room temperature and samples are filtered over glass fiber filters using a cell harvester. The non-specific binding determinant is 1 μM haloperidol. Saturation studies are conducted with [3H]YM-09151-2 in both the dopamine D2 and D4 receptor membranes on several different occasions. Data are analyzed using non-linear analysis programs. Compound affinities are determined using at least six different concentrations in triplicate for dopamine D2 receptor binding studies. IC50 values are converted to Ki values using the standard methods equation and in cases where more than one determination is made, the results are combined using an average weighting method.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

High-throughput drug screen identifies calcium and calmodulin inhibitors that reduce JCPyV infection [ Antiviral Res, 2024, 222:105817] PubMed: 38246207
The Food and Drug Administration-approved antipsychotic drug trifluoperazine, a calmodulin antagonist, inhibits viral replication through PERK-eIF2α axis [ Front Microbiol, 2022, 13:979904] PubMed: 36386620
In vitro effects of opicapone on activity of human UDP-glucuronosyltransferases isoforms [ Toxicol Lett, 2022, 367:3-8] PubMed: 35810997
Comparison of the drug-drug interactions potential of ibrutinib and acalabrutinib via inhibition of UDP-glucuronosyltransferase [ Toxicol Appl Pharmacol, 2021, 424:115595] PubMed: 34038714
In vitro inhibition of human UDP-glucuronosyltransferase (UGT) 1A1 by osimertinib, and prediction of in vivo drug-drug interactions [ Toxicol Lett, 2021, 348:10-17] PubMed: 34044055
A Low Dose of Aripiprazole Has the Strongest Sensitization Effect Among 19 Repositioned Bipolar Drugs in P-gp-overexpressing Drug-resistant Cancer Cells [ Anticancer Res, 2021, 41(2):687-697] PubMed: 33517273
Inhibition of human UDP-glucuronosyltransferase enzyme by Dabrafenib: Implications for drug-drug interactions [ Biomed Chromatogr, 2021, e5205] PubMed: 34192355
Inhibition of Human UDP-Glucuronosyltransferase Enzyme by Belinostat: Implications for Drug-Drug Interactions [ Toxicol Lett, 2020, S0378-4274(20)30494-X] PubMed: 33290829

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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