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TAK-041

Cat. No. M10682
TAK-041 Structure
Synonym:

NBI-1065846

Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 580  USD580 In stock
25mg USD 1080  USD1080 In stock
50mg USD 1620  USD1620 In stock
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Quality Control & Documentation
Biological Activity

TAK-041 is a first-in-class, selective GPR139 agonist with an EC50 of 22 nM. TAK-041 can be used to study negative symptoms of schizophrenia.

Chemical Information
Molecular Weight 392.33
Formula C18H15F3N4O3
CAS Number 1929519-13-0
Form Solid
Solubility (25°C) DMSO ≥ 60 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] Eugenii A Rabiner, et al. Neuropsychopharmacology. Endogenous dopamine release in the human brain as a pharmacodynamic biomarker: evaluation of the new GPR139 agonist TAK-041 with [ 11 C]PHNO PET

[2] Holly A Reichard, et al. J Med Chem. Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia

[3] Amin Kamel, et al. Drug Metab Dispos. In Vitro Metabolism of Slowly Cleared G Protein-Coupled Receptor 139 Agonist TAK-041 Using Rat, Dog, Monkey, and Human Hepatocyte Models (HepatoPac): Correlation with In Vivo Metabolism

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  Catalog
Abmole Inhibitor Catalog




Keywords: TAK-041, NBI-1065846 supplier, GPR/FFAR, inhibitors, activators


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