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Chemical Structure| 932986-18-0 Chemical Structure| 932986-18-0

Structure of Azoramide
CAS No.: 932986-18-0

Chemical Structure| 932986-18-0

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Azoramide is a modulator of the unfolded protein response (UPR) with antidiabetic activity.

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Product Details of Azoramide

CAS No. :932986-18-0
Formula : C15H17ClN2OS
M.W : 308.83
SMILES Code : CCCC(NCCC1=CSC(C2=CC=C(Cl)C=C2)=N1)=O
MDL No. :MFCD08009374
InChI Key :VYBFWKKCWTXCQX-UHFFFAOYSA-N
Pubchem ID :7518316

Safety of Azoramide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Related Pathways of Azoramide

pyroptosis

Isoform Comparison

Biological Activity

Description
Azoramide, a powerful, orally bioavailable small molecule, functions as a modulator of the unfolded protein response (UPR). It enhances ER protein folding capabilities and increases the capacity of ER chaperones, providing protection against ER stress. Furthermore, azoramide mitigates ER stress induced by PLA2G6 mutations by adjusting the unfolded protein response, boosts CERB signaling to restore mitochondrial function, and prevents apoptosis in dopaminergic (DA) neurons. Its efficacy extends to anti-diabetic activities[1].[2].

In Vitro:

Cell Line
Concentration Treated Time Description References
PLA2G6 D331Y mutant DA neurons 10 μM 5 days Azoramide significantly enhanced cell viability, inhibited the release of cytochrome c from mitochondria, decreased the cleaved level of caspase 3, and enhanced expression of CREB. PMC7028918
3T3-L1 adipocytes 30 µM 24 hours Azoramide significantly attenuated C. pneumoniae infection-induced lipolysis and FABP4 secretion. PMC7049972
HEK293 cells 25µM 4 hours Azoramide dose-dependently increased ASGR-Cluc secretion, indicating enhanced ER folding capacity. PMC5063051
INAD patient-derived NPCs 20 µM Azoramide significantly reduces LAMP2 levels and restores ATP levels, indicating its ability to alleviate lysosomal expansion and restore mitochondrial function. PMC9889087

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice ob/ob mice Oral Single implantation, lasted for six weeks Azoramide improved glucose metabolism in ob/ob mice, reducing fasting glucose and improving glucose tolerance. PMC5063051
mice Pla2g6KO/G373R INAD mouse model intracerebroventricular and intravenous injections 5 mg/kg BI 6727 and 0.1 mg/kg VCR Once weekly for 5 weeks Azoramide alleviates neurodegenerative phenotypes in INAD flies and reduces lysosomal expansion in INAD patient-derived NPCs. PMC9889087

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.19mL

3.24mL

1.62mL

32.38mL

6.48mL

3.24mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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