Free shipping on all orders over $ 500

TAK-418

Cat. No. M21127
TAK-418 Structure
Size Price Availability
Free Delivery on orders over USD 500 Bulk Inquiry?
Quality Control & Documentation
Biological Activity

TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. It is an orally administered CNS-permeable clinical candidate for the study of neurodevelopmental disorders, such as autism spectrum disorders.

Chemical Information
Molecular Weight 356.91
Formula C17H25ClN2O2S
CAS Number 1818252-53-7
Solubility (25°C) DMSO : 55 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yasushi Hattori, et al. Eur J Med Chem. Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects

[2] Rina Baba, et al. ACS Chem Neurosci. Investigating the Therapeutic Potential of LSD1 Enzyme Activity-Specific Inhibition by TAK-418 for Social and Memory Deficits in Rodent Disease Models

[3] Yihui Song, et al. Eur J Med Chem. Annual review of lysine-specific demethylase 1 (LSD1/KDM1A) inhibitors in 2021

[4] Wei Yin, et al. Br J Clin Pharmacol. Safety, pharmacokinetics and pharmacodynamics of TAK-418, a novel inhibitor of the epigenetic modulator lysine-specific demethylase 1A

[5] Rina Baba, et al. Sci Adv. LSD1 enzyme inhibitor TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models

Related Histone demethylase Products
INCB059872

INCB059872 is a potent, orally active, selective and irreversible inhibitor of lysine-specific demethylase 1 (LSD1) in myeloid leukemia.
KDM2A/7A-IN-1

KDM2A/7A-IN-1 is a first-in-class, selective, cell-permeable inhibitor of the histone lysine demethylase KDM2A/7A, with an IC50 value of 0.16 μM for KDM2A, 75-fold more selective than other JmjC lysine demethylases, and with no effect on methyltransferases or histone acetyltransferases. KDM2A was 75 times more selective than other JmjC lysine demethylases and had no effect on methyltransferases and histone acetyltransferases.
NCD38 TFA

NCD38 TFA is a LSD1-selective inhibitor.
LSD1-IN-26

LSD1-IN-26 is a potent LSD1 inhibitor, with an IC50 of 25.3 nM.
JMJD6-IN-1

JMJD6-IN-1 is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM.
  Catalog
Abmole Inhibitor Catalog




Keywords: TAK-418 supplier, Histone demethylase, inhibitors, activators

 
Get to Know Us
Customer Support
Resources
Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.