Free shipping on all orders over $ 500

Vafidemstat

Cat. No. M28239
Vafidemstat Structure
Synonym:

ORY-2001

Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.

Chemical Information
Molecular Weight 336.39
Formula C19H20N4O2
CAS Number 1357362-02-7
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic)
Storage Powder -20°C
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] Mehak Saba Lone, et al. J Biomol Struct Dyn. Design, synthesis and evaluation of 5-chloro-6-methylaurone derivatives as potential anti-cancer agents

[2] Beatrice Noce, et al. Front Pharmacol. LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

[3] Fernando Cavalcanti, et al. Pharmaceutics. Efficacy of Vafidemstat in Experimental Autoimmune Encephalomyelitis Highlights the KDM1A/RCOR1/HDAC Epigenetic Axis in Multiple Sclerosis

[4] Rosa María Antonijoan, et al. CNS Drugs. First-in-Human Randomized Trial to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of the KDM1A Inhibitor Vafidemstat

[5] Tamara Maes, et al. PLoS One. Modulation of KDM1A with vafidemstat rescues memory deficit and behavioral alterations

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: Vafidemstat, ORY-2001 supplier, Histone demethylase, inhibitors, activators


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