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Asivatrep

Cat. No. M10783
Asivatrep  Structure
Synonym:

PAC-14028

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Quality Control
  • Current batch:
  • Purity >95%
  • COA
  • MSDS
Biological Activity

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 491.47
Formula C21H22F5N3O3S
CAS Number 1005168-10-4
Purity >95%
Solubility DMSO ≥ 20 mg/mL
Storage at -20°C
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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Keywords: Asivatrep , PAC-14028 supplier, TRP Channel, inhibitors

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