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AF38469

Cat. No. M1558
AF38469 Structure
Synonym:

AF-38469

Size Price Availability Quantity
2mg USD 180  USD180 In stock
5mg USD 260  USD260 In stock
10mg USD 420  USD420 In stock
25mg USD 825  USD825 In stock
50mg USD 1320  USD1320 In stock
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Quality Control & Documentation
Biological Activity

AF38469 is an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin with IC50 of 330 nM.

Chemical Information
Molecular Weight 324.25
Formula C15H11F3N2O3
CAS Number 1531634-31-7
Solubility (25°C) 43 mg/mL in DMSO
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] Fangfang Gao, et al. The Membrane Protein Sortilin Can Be Targeted to Inhibit Pancreatic Cancer Cell Invasion

[2] Wei Yang, et al. Sortilin promotes glioblastoma invasion and mesenchymal transition through GSK-3β/β-catenin/twist pathway

[3] Cheng Chen, et al. Hepatocyte sortilin 1 knockout and treatment with a sortilin 1 inhibitor reduced plasma cholesterol in Western diet-fed mice

[4] Sara Rhost, et al. Sortilin inhibition limits secretion-induced progranulin-dependent breast cancer progression and cancer stem cell expansion

[5] Tenna Juul Schrder, et al. The identification of AF38469: an orally bioavailable inhibitor of the VPS10P family sorting receptor Sortilin

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Keywords: AF38469, AF-38469 supplier, Neurotensin Receptor, inhibitors, activators


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