>>Signaling Pathways>> Chromatin/Epigenetics>> Histone Demethylases>>T-448

T-448

Catalog No.GC65456

T-448은 22nM의 IC50을 갖는 라이신 특이적 데메틸라제 1(LSD1, H3K4 데메틸라제)의 특이적 경구 활성 및 비가역적 억제제입니다.

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T-448 Chemical Structure

Cas No.: 1597426-53-3

Size 가격 재고 수량
1mg
US$495.00
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5mg
US$882.00
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10mg
US$1,350.00
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Sample solution is provided at 25 µL, 10mM.

Description of T-448

T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons[1].

T-448 enhances the levels of H3K4 methylation, increased mRNA expression of neural plasticity-related genes including brain derived neurotrophic factor (Bdnf), and ameliorated learning dysfunction[1].

T-448 has minimal impact on the LSD1-GFI1B complex and a superior hematological safety profile in mice via the generation of a compact formyl-FAD adduct. T-448 increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction[1].T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg[1].

[1]. Matsuda S, et al. T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice. Neuropsychopharmacology. 2018 Dec 22.

Chemical Properties of T-448

Cas No. 1597426-53-3 SDF
Formula C17H20N4OS.1/2C4H4O4 M.Wt 386.5
Solubility DMSO : 16.67 mg/mL (43.13 mM; Need ultrasonic) Storage Store at -20°C, stored under nitrogen
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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of T-448

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1 mg 5 mg 10 mg
1 mM 2.5873 mL 12.9366 mL 25.8732 mL
5 mM 0.5175 mL 2.5873 mL 5.1746 mL
10 mM 0.2587 mL 1.2937 mL 2.5873 mL
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In vivo Formulation Calculator (Clear solution) of T-448

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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 ddH2O, 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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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