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O-304

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O-304 Basic information

Product Name:
O-304
Synonyms:
  • O-304
  • O-304 1261289-04-6
  • 4-chloro-N-(2-(4-chlorobenzyl)-3-oxo-2,3-dihydro-1,2,4-thiadiazol-5-yl)benzamide
  • CS-2682
  • 0 304
  • O-304;0 304
  • Benzamide, 4-chloro-N-[2-[(4-chlorophenyl)methyl]-2,3-dihydro-3-oxo-1,2,4-thiadiazol-5-yl]-
  • O 304,AMPK,O-304,inhibit,Inhibitor,AMP-activated protein kinase,O304
CAS:
1261289-04-6
MF:
C16H11Cl2N3O2S
MW:
380.25
Mol File:
1261289-04-6.mol
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O-304 Chemical Properties

Density 
1.50±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:30): 0.03 mg/ml; Ethanol: slightly soluble
form 
A crystalline solid
pka
7.81±0.20(Predicted)
color 
White to off-white
InChI
InChI=1S/C16H11Cl2N3O2S/c17-12-5-1-10(2-6-12)9-21-16(23)20-15(24-21)19-14(22)11-3-7-13(18)8-4-11/h1-8H,9H2,(H,19,20,22,23)
InChIKey
WEDWLYRQKUTOAX-UHFFFAOYSA-N
SMILES
C(NC1SN(CC2=CC=C(Cl)C=C2)C(=O)N=1)(=O)C1=CC=C(Cl)C=C1
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O-304 Usage And Synthesis

Uses

O-304 is a first-in-class, orally available pan-AMPK activator, which increases AMPK activity by suppressing the dephosphorylation of pAMPK. O-304 exhibits a great potential as a agent to treat type 2 diabetes (T2D) and associated cardiovascular complications [1][2].

in vivo

O-304 increases glucose uptake in skeletal muscle, reduces β cell stress, and promotes β cell rest in diet-induced obese mice. O-304 reduces fasting plasma glucose levels and homeostasis model assessment of insulin resistance (HOMA-IR) in a proof-of-concept phase IIa clinical trial in type 2 diabetes (T2D) patients on Metformin[2].

References

[1] Periodic Reporting for period 1-AMPK-DIAB (A small molecule AMP activated protein kinase (AMPK) activator, denoted O304, as a novelinnovative drug for the treatment of type 2 diabetes).

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