| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
0.59 μM (ATF6α)[1]
Ceapin-A7 targets activating transcription factor 6α (ATF6α), one of the three branches of the unfolded protein response (UPR). ATF6α is a transcription factor that is activated in response to ER stress and promotes cell survival. Ceapin-A7 inhibits ATF6α with an IC50 of 0.59 μM. It is selective for ATF6α over ATF6β (at 18.9 μM) and does not inhibit SREBP activation, the IRE1 branch, or the PERK branch of the UPR. |
|---|---|
| ln Vitro |
Ceapin-A7 increases a cell's sensitivity to ER stress [1]. ATF6α but not ATF6β is selectively inhibited by ceapin (0.6–18.9 μM; 4.5 hours)[1].
In vitro studies demonstrate that Ceapin-A7 selectively inhibits ATF6α activation in response to ER stress without inhibiting ATF6β or SREBP activation. In U2-OS cells, the compound inhibits ER stress-induced upregulation of BiP. Ceapin-A7 (0.6-18.9 μM; 4.5 hours) selectively inhibits ATF6α but not ATF6β. The compound sensitizes cells to ER stress. It does not affect the IRE1 or PERK branches of the UPR. |
| ln Vivo |
No detailed in vivo activity data has been published for Ceapin-A7. The compound has been primarily characterized in vitro as a research tool for studying ATF6α signaling and the unfolded protein response. Its ability to selectively inhibit ATF6α suggests that it could have potential for in vivo applications in diseases involving ER stress, such as neurodegenerative disorders, cancer, and metabolic diseases.
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| Enzyme Assay |
The ATF6α inhibitory activity of Ceapin-A7 can be assessed using reporter assays. In a typical assay, cells are transfected with an ATF6α-responsive luciferase reporter construct and treated with varying concentrations of Ceapin-A7. ER stress is induced using agents such as thapsigargin or tunicamycin. The inhibition of ATF6α activation is measured by luciferase activity, and the IC50 (0.59 μM) is calculated. The selectivity for ATF6α over ATF6β is assessed using similar assays with ATF6β-responsive reporters.
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| Cell Assay |
The cellular activity of Ceapin-A7 is assessed using U2-OS cells or other cell lines. Cells are treated with Ceapin-A7 (0.6-18.9 μM; 4.5 hours). ER stress is induced using thapsigargin or tunicamycin. ATF6α activation is assessed by measuring the cleavage and nuclear translocation of ATF6α by Western blotting or immunofluorescence. BiP (an ATF6α target gene) expression is measured by qPCR or Western blotting. Cell viability is assessed using MTT assays.
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| Animal Protocol |
No detailed in vivo animal model data has been published for Ceapin-A7. The compound has been primarily characterized in vitro as a research tool for studying ATF6α signaling. Future studies may involve the use of mouse models of ER stress-related diseases to assess the in vivo efficacy of Ceapin-A7. Such studies would be essential to confirm the compound's ability to modulate ATF6α signaling in a physiological setting.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data has been published for Ceapin-A7. The compound has a molecular weight of approximately 360 g/mol. It is soluble in DMSO. Further studies would be needed to characterize its absorption, distribution, metabolism, and excretion properties, including oral bioavailability, plasma protein binding, clearance, and half-life.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published for Ceapin-A7. As an ATF6α inhibitor, it may have on-target effects on the unfolded protein response in normal cells. Comprehensive toxicology studies would be required to evaluate its safety profile for potential therapeutic development. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Ceapin-A7 (CAS# 2323027-38-7) is a selective and highly potent inhibitor of ATF6α with an IC50 of 0.59 μM in a reporter assay. It selectively inhibits ATF6α activation in response to ER stress without inhibiting ATF6β, SREBP, IRE1, or PERK. In U2-OS cells, the compound inhibits ER stress-induced upregulation of BiP. Ceapin-A7 sensitizes cells to ER stress. It is used to explore ATF6α activation mechanisms and its role in pathological settings.
|
| Molecular Formula |
C20H12F6N4O3
|
|---|---|
| Molecular Weight |
470.3247
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| Exact Mass |
470.081
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| CAS # |
2323027-38-7
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| PubChem CID |
154730128
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
694
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
FC(C1C=C(C(F)(F)F)C=CC=1CN1C=C(C=N1)NC(C1C=C(C2=CC=CO2)ON=1)=O)(F)F
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| InChi Key |
UJTDYOXTXGBHEG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H12F6N4O3/c21-19(22,23)12-4-3-11(14(6-12)20(24,25)26)9-30-10-13(8-27-30)28-18(31)15-7-17(33-29-15)16-2-1-5-32-16/h1-8,10H,9H2,(H,28,31)
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| Chemical Name |
N-[1-[[2,4-bis(trifluoromethyl)phenyl]methyl]pyrazol-4-yl]-5-(furan-2-yl)-1,2-oxazole-3-carboxamide
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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 |
| 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) |
DMSO : 100 mg/mL (212.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.32 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1262 mL | 10.6311 mL | 21.2621 mL | |
| 5 mM | 0.4252 mL | 2.1262 mL | 4.2524 mL | |
| 10 mM | 0.2126 mL | 1.0631 mL | 2.1262 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.
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