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Asivatrep

Cat. No. M10783
Asivatrep  Structure
Synonym:

PAC-14028

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Quality Control & Documentation
Biological Activity

Asivatrep (PAC-14028) is a highly selective transient receptor potential vanilla acid subtype 1 (TRPV1) antagonist.

Chemical Information
Molecular Weight 491.47
Formula C21H22F5N3O3S
CAS Number 1005168-10-4
Solubility (25°C) DMSO ≥ 20 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] Chun Wook Park, et al. J Allergy Clin Immunol. Asivatrep, a TRPV1 antagonist, for the topical treatment of atopic dermatitis: Phase 3, randomized, vehicle-controlled study (CAPTAIN-AD)

[2] Jin Kyu Choi, et al. Regul Toxicol Pharmacol. A TRPV1 antagonist, PAC-14028 does not increase the risk of tumorigenesis in chemically induced mouse skin carcinogenesis

[3] Sabrina Bartolucci, et al. J Cutan Med Surg. Recent Therapeutic Advances in Pruritus Management for Atopic Dermatitis Patients: A Welcome Addition of Asivatrep to Our Arsenal of Future Topical Treatments

[4] Ji-Hae Lee, et al. J Dermatol Sci. A novel, topical, nonsteroidal, TRPV1 antagonist, PAC-14028 cream improves skin barrier function and exerts anti-inflammatory action through modulating epidermal differentiation markers and suppressing Th2 cytokines in atopic dermatitis

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