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Purity: ≥98%
Azoramide is a small-molecule modulator of the unfolded protein response (UPR) and an ER stress alleviator that is reported to have antidiabetic activity. It can improve ER protein-folding ability and activates ER chaperone capacity to protect cells against ER stress. Azoramide also displayed potent antidiabetic efficacy in two mouse models with obesity by improving by improving peripheral insulin sensitivity and pancreatic β-cell function. Therefore, azoramide has the potential to be developed as a drug for type 2 diabete. In addition, a recent study showed that azoramide may serve as an antagonist against GLP-1R in MSC (mesenchymal stem cells) lineage determination, and azoramide favors adipogenesis against osteogenesis through inhibiting the GLP-1 receptor-PKA-β-catenin pathway.
| Targets |
UPR
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| Cell Assay |
In either the absence or presence of 20 mM azoramide, INS1 cells are treated for 60 hours with 25 mM glucose and 500 mM palmitate (G/P). Using the CellTiter-Glo cell viability assay system, viability is evaluated after incubation.
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| References |
| Molecular Formula |
C15H17CLN2OS
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| Molecular Weight |
308.83
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| Exact Mass |
308.075
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| Elemental Analysis |
C, 58.34; H, 5.55; Cl, 11.48; N, 9.07; O, 5.18; S, 10.38
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| CAS # |
932986-18-0
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CCCC(=O)NCCC1=CSC(=N1)C2=CC=C(C=C2)Cl
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| InChi Key |
VYBFWKKCWTXCQX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H17ClN2OS/c1-2-3-14(19)17-9-8-13-10-20-15(18-13)11-4-6-12(16)7-5-11/h4-7,10H,2-3,8-9H2,1H3,(H,17,19)
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| Chemical Name |
N-[2-[2-(4-chlorophenyl)-1,3-thiazol-4-yl]ethyl]butanamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Reduced BMP2-induced bone formation in azoramide-treated mice.Stem Cell Res Ther. 2018; 9: 57. |
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Inhibited osteogenic differentiation potential of C3H10T1/2 cells with azoramide treatment in vitro.Stem Cell Res Ther. 2018; 9: 57. |
Enhanced adipogenic differentiation potential of C3H10T1/2 cells and mouse-derived MSCs with azoramide treatment in vitro.Stem Cell Res Ther. 2018; 9: 57. |
Ex-4 treatment attenuated azoramide effects on suppressing C3H10T1/2 cell osteoblast differentiation and promoting their differentiation into adipocytes.Stem Cell Res Ther. 2018; 9: 57. |
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GLP-1R silencing abolished the azoramide (Azo) regulatory effects of suppressing C3H10T1/2 cell osteoblast differentiation and promoting their differentiation into adipocytes.Stem Cell Res Ther. 2018; 9: 57. |
Decreased expression levels of protein kinase A (PKA) with azoramide (Azo) treatment.Stem Cell Res Ther. 2018; 9: 57. |
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Image depicting the main facts observed of azoramide pre-treatment on ER homeostasis.Ann Transl Med. 2016 Oct; 4(Suppl 1): S45 |
Azoramideregulates ER folding and secretion capacity without inducing ER stress.Sci Transl Med.2015 Jun 17;7(292):292ra98. |
Azoramideprotects against chemically-induced ER stress in vitro.Sci Transl Med.2015 Jun 17;7(292):292ra98. |
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Azoramideinduces weight loss, changes in energy expenditure and improved metabolic profile in mice with diet-induced obesity.Sci Transl Med.2015 Jun 17;7(292):292ra98. |
Azoramideimproves ER function, insulin secretion and survival in beta cells.Sci Transl Med.2015 Jun 17;7(292):292ra98. |
Azoramidetreatment alters ER calcium homeostasis.Sci Transl Med.2015 Jun 17;7(292):292ra98. |
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Azoramidereduces ER stress and improves metabolism inob/obmice.Sci Transl Med.2015 Jun 17;7(292):292ra98. |
Reporter systems monitor ER chaperone availability and activity.Sci Transl Med.2015 Jun 17;7(292):292ra98. |
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