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Porcupine-IN-1

Cat. No. M10124
Porcupine-IN-1 Structure
Synonym:

Porcn-IN-1

Size Price Availability Quantity
5mg USD 150  USD150 In stock
10mg USD 245  USD245 In stock
25mg USD 495  USD495 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Porcupine-IN-1 is a potent porcupine inhibitor with IC50 value of 0.5±0.2 nM. Porcupine-IN-1 is as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Porcupine-IN-1 potently inhibits the secretion of Wnt3A.

In vivo, Porcupine-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg). It exhibits high clearance when treated with mouse microsomes (109 mL/min/kg).

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 410.44
Formula C25H19FN4O
CAS Number 2036044-77-4
Purity >99%
Solubility DMSO ≥ 90 mg/mL
Storage at -20°C
References

[1] Zhixiang Xu, et al. Bioorg Med Chem. Design, synthesis, and evaluation of novel porcupine inhibitors featuring a fused 3-ring system based on the 'reversed' amide scaffold

  Catalog
Abmole Inhibitor Catalog




Keywords: Porcupine-IN-1, Porcn-IN-1 supplier, Porcupine, inhibitors

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