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Difelikefalin (CR-845; FE-202845) TFA

Cat. No. M10432
Difelikefalin (CR-845; FE-202845) TFA Structure
Synonym:

Disomotide; KORSUVA; MR13A9 TFA

Size Price Availability Quantity
5mg USD 310  USD310 In stock
10mg USD 500  USD500 In stock
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Quality Control & Documentation
Biological Activity

Difelikefalin (CR-845; FE-202845) TFA is a synthetic peptide and the first-in-class, peripherally-restricted, selective agonist of the κ-opioid receptor (KOR) for studies related to pruritus.

Chemical Information
Molecular Weight 793.87
Formula C36H53N7O6.C2HF3O2
CAS Number 1024828-77-0 (free base)
Solubility (25°C) Water 100 mg/mL
DMSO 90 mg/mL
Storage -20°C, dry, sealed
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] Steven Fishbane, et al. Kidney Int Rep. Randomized Controlled Trial of Difelikefalin for Chronic Pruritus in Hemodialysis Раt iеnts

[2] Steven Fishbane, et al. N Engl J Med. A рhasе 3 Trial of Difelikefalin in Hemodialysis Раt iеnts with Pruritus

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Keywords: Difelikefalin (CR-845; FE-202845) TFA, Disomotide; KORSUVA; MR13A9 TFA supplier, Opioid Receptor, inhibitors, activators


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