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AS 1269574

Cat. No. M6466
AS 1269574 Structure
Size Price Availability Quantity
5mg USD 82  USD82 In stock
10mg USD 140  USD140 In stock
25mg USD 270  USD270 In stock
50mg USD 430  USD430 In stock
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Quality Control & Documentation
Biological Activity

AS1269574 is a potent, orally active GPR119 agonist with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates the TRPA1 cation channel and stimulates glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induced pancreatic β cells to secrete glucose-dependent insulin only under high glucose conditions. AS1269574 has potential for type 2 diabetes research.

Chemical Information
Molecular Weight 308.17
Formula C13H14BrN3O
CAS Number 330981-72-1
Form Solid
Solubility (25°C) DMSO 30.82 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] Ashcroft and Gribble. TiPS. New windows on the mechanism of action of KATP channel openers.

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