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PF-4840154

Cat. No. M14283
PF-4840154 Structure
Size Price Availability Quantity
5mg USD 350  USD350 In stock
10mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.

Chemical Information
Molecular Weight 466.62
CAS Number 1332708-14-1
Solubility (25°C) DMSO 50 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] Clara Hoebart, et al. No functional TRPA1 in cardiomyocytes

[2] Amrita Samanta, et al. Structural insights into the molecular mechanism of mouse TRPA1 activation and inhibition

[3] Thomas Ryckmans, et al. Design and pharmacological evaluation of PF-4840154, a non-electrophilic reference agonist of the TrpA1 channel

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