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GDC-0334

Cat. No. M21130
GDC-0334  Structure
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Biological Activity

GDC-0334 is a TRPA1 antagonist for the treatment of TRPA1-mediated disease and is an oral candidate compound for the study of asthma.

Chemical Information
Molecular Weight 609.49
Formula C24H19F8N5O3S
CAS Number 1984824-54-5
Solubility (25°C) N/A
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] Chun-Wan Yen, et al. Int J Pharm. Impact of surfactant selection and incorporation on in situ nanoparticle formation from amorphous solid dispersions

[2] Phyllis Chan, et al. Clin Transl Sci. Translational and pharmacokinetic-pharmacodynamic application for the clinical development of GDC-0334, a novel TRPA1 inhibitor

[3] Alessia Balestrini, et al. J Exp Med. A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment

[4] Huifen Chen, et al. Expert Opin Ther Pat. Transient receptor potential ankyrin 1 (TRPA1) antagonists: a patent review (2015-2019)

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