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AZD7687

Cat. No. M2722
AZD7687 Structure
Size Price Availability
5mg USD 220  USD220 Out of stock
10mg USD 390  USD390 Out of stock
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Biological Activity

AZD7687 is a reversible and selective DGAT1 inhibitor with IC50 value of 80 nM. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship. AZD7687 shows inhibition of acyl-CoA:cholesterol acetyltransferase (79% at 10 μM), fatty acid amide hydrolase (IC50 = 3.7 μM), muscarinic M2 receptor (IC50 = 80.5 μM), and phosphodiesterase PDE10A1 (IC50 = 5.5 μM).

Chemical Information
Molecular Weight 367.44
Formula C21H25N3O3
CAS Number 1166827-44-6
Solubility (25°C) DMSO 40 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] Pablo Morentin Gutierrez, et al. Evolving data analysis of an Oral Lipid Tolerance Test toward the standard for the Oral Glucose Tolerance Test: Cross species modeling effects of AZD7687 on plasma triacylglycerol

[2] Eike Floettmann, et al. Pharmacological inhibition of DGAT1 induces sebaceous gland atrophy in mouse and dog skin while overt alopecia is restricted to the mouse

[3] H Denison, et al. Diacylglycerol acyltransferase 1 inhibition with AZD7687 alters lipid handling and hormone secretion in the gut with intolerable side effects: a randomized clinical trial

[4] Jonas G Barlind, et al. Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687)

[5] H Denison, et al. Proof of mechanism for the DGAT1 inhibitor AZD7687: results from a first-time-in-human single-dose study

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Keywords: AZD7687 supplier, DGAT, inhibitors, activators

 
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