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Difamilast

Cat. No. M10435
Difamilast Structure
Synonym:

OPA-15406

Size Price Availability Quantity
5mg USD 400  USD400 In stock
10mg USD 640  USD640 In stock
25mg USD 1280  USD1280 In stock
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Quality Control & Documentation
Biological Activity

Difamilast (OPA-15406) is a topical, highly selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor. Difamilast has particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast (OPA-15406) improves skin condition in relevant animal models of AD.

Chemical Information
Molecular Weight 446.44
Formula C23H24F2N2O5
CAS Number 937782-05-3
Solubility (25°C) DMSO 90 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] Jusleen Ahluwalia, et al. Dгυgs. Phosphodiesterase 4 Inhibitor Therapies for Atopic Dermatitis: Progress and Outlook

[2] Jon M Hanifin, et al. J Am Acad Dermatol. OPA-15406, a novel, topical, nonsteroidal, selective phosphodiesterase-4 (PDE4) inhibitor, in the treatment of adult and adolescent patients with mild to moderate atopic dermatitis (AD): A phase-II randomized, double-blind, placebo-controlled study

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  Catalog
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