2. Apoptosis
    NF-κB
    Metabolic Enzyme/Protease
    Immunology/Inflammation
  3. Apoptosis
    Reactive Oxygen Species
    Caspase
    Bcl-2 Family
    Mitochondrial Metabolism
  4. Azoramide

Azoramide 

Cat. No.: HY-18705 Purity: 98.63%
COA Handling Instructions

Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity.

For research use only. We do not sell to patients.

Azoramide Chemical Structure

Azoramide Chemical Structure

CAS No. : 932986-18-0

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10 mM * 1 mL in DMSO USD 61 In-stock
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10 mg USD 66 In-stock
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25 mg USD 132 In-stock
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50 mg USD 209 In-stock
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100 mg USD 385 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Azoramide purchased from MCE. Usage Cited in: Stem Cell Res Ther. 2018 Mar 9;9(1):57.  [Abstract]

    Western blot of Runx2 protein in C3H10T1/2 cells subjected to 15 μM Azoramide.

    View All Caspase Isoform Specific Products:

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    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11

    View All Bcl-2 Family Isoform Specific Products:

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    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity[1][2].

    In Vitro

    Azoramide (0.01-100 µM; 0-24 h; Huh7 cells) regulates ER folding and secretion capacity without inducing ER stress[1].
    Azoramide (15 µM; 2-16 h; Huh7 cells) protects cells from induced ER stress. Azoramide counteracts Tunicamycin (Tm, HY-A0098)-induced ATF6LD-Cluc secretion and Tm-induced decrease of ASGR-Cluc secretion. Azoramide suppresses Tm-induced GRP78 and CHOP protein expression[1].
    Azoramide (15 µM; 2-16 h; Hepa 1-6 cells) alters ER calcium homeostasis and retains a greater fraction of Ca2+ in the ER[1].
    Azoramide (0-10 µM; 5 d) attenuates loss of PLA2G6D331Y/D331Y iPSC-derived midbrain DA neurons[2].
    Azoramide (10 µM; 5 d) reduces the increase in ROS and ameliorates the decline in mitochondrial membrane potential in PLA2G6D331Y/D331Y midbrain DA neurons[2].
    Azoramide (10 µM; 0-30 d) suppresses mitochondrial fragmentation in PLA2G6D331Y/D331Y midbrain DA neurons[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[2]

    Cell Line: DA neurons
    Concentration: 0, 0.1, 0.3, 1, 3, and 10 µM
    Incubation Time: 5 days
    Result: Enhanced cell viability with 27 and 39% for 3 and 10 μM, respectively.

    Western Blot Analysis[2]

    Cell Line: DA neurons
    Concentration: 10 μM
    Incubation Time: 24 hours
    Result: Decreased the cleaved level of caspase 3 and the ratio of Bax/Bcl2 in PLA2G6 mutant neurons.
    Enhanced expression of CREB in PLA2G6 mutant neurons.

    Western Blot Analysis[2]

    Cell Line: DA neurons
    Concentration: 10 μM
    Incubation Time: 30 days
    Result: Suppressed increased expression of UPR proteins, elevated the decreased expression level of mfn1, and inhibited the elevated expression levels of DRP1 and Fis1 in PLA2G6 mutant neurons
    In Vivo

    Azoramide (150 mg/kg; p.o.; daily, for 7 d; Huh7 cells; ob/ob mice) improves glucose homeostasis in mice with genetic obesity and preserves beta cell function and survival during metabolic ER stress[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male ob/ob mice (9-12 weeks of age)[1]
    Dosage: 150 mg/kg
    Administration: Oral administration; daily, for 7 days
    Result: Reduces ER stress and improves metabolism in ob/ob mice.
    Increased the levels of Pdx1 mRNA and improved beta cell function.
    Molecular Weight

    308.83

    Appearance

    Solid

    Formula

    C15H17ClN2OS
    CAS No.
    SMILES

    CCCC(NCCC1=CSC(C2=CC=C(Cl)C=C2)=N1)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 30 mg/mL (97.14 mM)

    Ethanol : < 1 mg/mL (ultrasonic) (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2380 mL 16.1901 mL 32.3803 mL
    5 mM 0.6476 mL 3.2380 mL 6.4761 mL
    10 mM 0.3238 mL 1.6190 mL 3.2380 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 98.63%

    COA (244 KB) HNMR (260 KB) LCMS (100 KB)

    Handling Instructions (2659 KB)
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Azoramide932986-18-0ApoptosisReactive Oxygen SpeciesCaspaseBcl-2 FamilyMitochondrial Metabolismunfolded protein responseER protein foldER chaperone capacityCERB signalingmitochondrial functionDA neuronsantidiabeticInhibitorinhibitorinhibit

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