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Chemical Structure| 2323027-38-7 Chemical Structure| 2323027-38-7

Structure of Ceapin-A7
CAS No.: 2323027-38-7

Chemical Structure| 2323027-38-7

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Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress with IC50 of 0.59 μM.

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Product Details of Ceapin-A7

CAS No. :2323027-38-7
Formula : C20H12F6N4O3
M.W : 470.32
SMILES Code : O=C(C1=NOC(C2=CC=CO2)=C1)NC3=CN(CC4=CC=C(C(F)(F)F)C=C4C(F)(F)F)N=C3
MDL No. :MFCD31567506
InChI Key :UJTDYOXTXGBHEG-UHFFFAOYSA-N
Pubchem ID :154730128

Safety of Ceapin-A7

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CD4+T cells 6µM 1 hour Inhibit ATF6 signaling pathway and reduce the differentiation of Th17 cells PMC11605992
PBMCs 6µM 1 hour Inhibit ATF6 signaling pathway and reduce the expression of ATF6α PMC11605992
Bovine pulmonary artery endothelial cells (BPAEC) 20 μM 16, 20, 24, 36, 48 hours To evaluate the effects of Ceapin-A7 on ATF6 activation and Cofilin phosphorylation. Ceapin-A7 reduced ATF6 activation and Cofilin phosphorylation. PMC10413362
Bovine pulmonary artery endothelial cells (BPAEC) 15 μM 24 hours To evaluate the effects of Ceapin-A7 on LPS-induced endothelial barrier dysfunction. Ceapin-A7 enhanced LPS-induced VE-cadherin internalization and barrier dysfunction. PMC10413362
Bovine pulmonary artery endothelial cells (BPAEC) 10, 15, 20 μM 24 hours To evaluate the effects of Ceapin-A7 on ATF6 activation and Cofilin phosphorylation. Ceapin-A7 decreased ATF6 activation and Cofilin phosphorylation. PMC10413362
RA FLSs 1, 2, or 5 µM 24 hours Inhibited BIRC3 expression PMC9590309
Human chondrocytes 500 nM 24 hours Inhibited ATF6 activation and reduced FGF2 expression PMC8281657
Bovine pulmonary artery endothelial cells (BPAEC) 1–150 μM 24 hours and 48 hours To evaluate the effects of Ceapin-A7 on cell viability. Moderate doses (1–25 μM) were non-toxic, while higher doses (50–150 μM) reduced cell viability. PMC10413362
A549 cells 6 μM 24 to 72 hours Inhibited ATF6 cleavage, reduced virus titer PMC8265652
786-O cells 20 µM 5 hours Inhibited ATF6 activation, reversed the increased expression of PINK1 and BNIP3 caused by NR3C1 knockdown. PMC10560440
ACHN cells 20 µM 5 hours Inhibited ATF6 activation, reversed the increased expression of PINK1 and BNIP3, and the decreased expression of LC3 and increased expression of P62 caused by NR3C1 knockdown. PMC10560440

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
DBA/1J mice Collagen-induced arthritis (CIA) model Intraperitoneal injection 10 mg/kg Three times per week from days 22 to days 45 Reduced arthritis severity and bone erosion PMC9590309
SKG mice Ankylosing spondylitis model Oral administration in drinking water 1 mM Continuous administration until the end of the experiment Reduced the number of vessels and osteophytes, inhibited angiogenesis-osteogenesis coupling PMC8281657

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.63mL

2.13mL

1.06mL

21.26mL

4.25mL

2.13mL

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