Sjc 13
Sjc 13 is an inhibitor of E-selectin and VCAM-1, with IC50 values of 150 μg/mL and 115 μg/mL, respectively. Sjc 13 prevents neutrophil migration and adhesion by selectively inhibiting the expression and mRNA synthesis of E-selectin and VCAM-1 in LPS-stimulated endothelial cells, thereby protecting against LPS-induced lethal shock. Sjc 13 is applicable to the study of septic shock.
For research use only. We do not sell to patients.
- CAS No.: 133669-72-4
- Formula: C17H18N3NaO4
- Molecular Weight:351.33
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All DNA/RNA Synthesis Isoforms
More
Biological Activity
Description
IC50 & Target
[2]|
E-selectin 150 μg/mL (IC50) |
VCAM-1 115 μg/mL (IC50) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
150 μg/mL
|
Inhibition of LPS-induced E-selectin expression on human umbilical vein endothelial cells (HUVEC) assessed by cellular enzyme-linked immunosorbent assay (cell-ELISA) following 1 h pretreatment with Sjc 13 prior to 4 h LPS stimulation.
Inhibition of LPS-induced E-selectin expression on human umbilical vein endothelial cells (HUVEC) assessed by cellular enzyme-linked immunosorbent assay (cell-ELISA) following 1 h pretreatment with Sjc 13 prior to 4 h LPS stimulation.
|
8737744 |
| HUVEC | IC50 |
760 μg/mL
|
Inhibition of LPS-induced ICAM-1 expression on human umbilical vein endothelial cells (HUVEC) assessed by cellular enzyme-linked immunosorbent assay (cell-ELISA) following 1 h pretreatment with Sjc 13 prior to 24 h LPS stimulation.
Inhibition of LPS-induced ICAM-1 expression on human umbilical vein endothelial cells (HUVEC) assessed by cellular enzyme-linked immunosorbent assay (cell-ELISA) following 1 h pretreatment with Sjc 13 prior to 24 h LPS stimulation.
|
8737744 |
| HUVEC | IC50 |
115 μg/mL
|
Inhibition of LPS-induced VCAM-1 expression on human umbilical vein endothelial cells (HUVEC) assessed by cellular enzyme-linked immunosorbent assay (cell-ELISA) following 1 h pretreatment with Sjc 13 prior to 24 h LPS stimulation.
Inhibition of LPS-induced VCAM-1 expression on human umbilical vein endothelial cells (HUVEC) assessed by cellular enzyme-linked immunosorbent assay (cell-ELISA) following 1 h pretreatment with Sjc 13 prior to 24 h LPS stimulation.
|
8737744 |
In Vitro
Sjc 13 (1 mg/mL; 1 h pre-incubation, 4 h/24 h Lipopolysaccharides, from E. coli O111:B4 (LPS) (HY-D1056A1) stimulation) completely inhibits the adhesion of HL60 cells to LPS-stimulated HUVECs at 4 h after stimulation, but exerts no effect on adhesion at 24 h after stimulation[2].
Sjc 13 (1 mg/mL; 1 h pre-incubation, 4 h/24 h LPS stimulation) inhibits LPS-induced expression of E-selectin (expression reduced by 95%) and VCAM-1 (expression reduced by 94%) on human umbilical vein endothelial cells (HUVEC), but does not affect ICAM-1 expression and has no impact on basal adhesion molecule levels[2].
Sjc 13 (62.5-1000 μg/mL; 1 h pre-incubation, 4 h/24 h LPS stimulation) exerts a stronger inhibitory effect on LPS-induced expression of E-selectin (IC50 = 150 μg/mL) and VCAM-1 (IC50 = 115 μg/mL) in human umbilical vein endothelial cells (HUVEC) than on LPS-induced ICAM-1 expression (IC50 = 760 μg/mL), and exhibits concentration-dependent activity in the range of 62.5 to 1000 μg/mL[2].
Sjc 13 (1 mg/mL; 1 h pre-incubation, 4 h LPS stimulation) inhibits LPS-induced mRNA expression of E-selectin and VCAM-1 in human umbilical vein endothelial cells (HUVEC), but does not affect LPS-induced ICAM-1 mRNA levels[2].
Sjc 13 inhibits the adhesion of HL60 cells to LPS-stimulated HUVECs, and selectively suppresses the expression and mRNA synthesis of E-selectin and VCAM-1 in LPS-stimulated HUVECs when administered 1-2 h after LPS stimulation; its activity is lost if it is added 2 h after LPS stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human umbilical vein endothelial cells (HUVEC)
-
Concentration:1 mg/mL
-
Incubation Time:1 h pre-incubation
-
Result:Did not show any cytotoxicity to HUVEC.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c (7-week-old female, specific pathogen-free, septic shock model via intravenous LD100 LPS injection)[1]
-
Dosage:1 mg/kg (pretreatment); 3 mg/kg (pretreatment); 10 mg/kg (pretreatment; 5 min post-LPS; 30 min post-LPS; 1 h post-LPS; 2 h post-LPS)
-
Administration:i.v.; single dose
-
Result:Provided partial protection against LPS-induced lethality at 1 mg/kg when administered 5 min prior to LPS.
Prevented LPS-induced lethality at 3 mg/kg and 10 mg/kg when administered 5 min prior to LPS.
Protected against LPS-induced lethality at 10 mg/kg when administered 5 min, 30 min, or 1 h after LPS.
Showed little protection against LPS-induced lethality at 10 mg/kg when administered 2 h after LPS.
Reduced lung MPO activity to 0.207 OD at 450 nm at 10 mg/kg when administered 5 min prior to LPS.
Greatly reduced neutrophil margination, aggregation in microvasculature, and intra-alveolar infiltration in lung tissue at 10 mg/kg when administered 5 min prior to LPS.
Did not significantly reduce lung MPO activity at 1 mg/kg when administered 5 min prior to LPS.
Chemical Information
-
CAS No. 133669-72-4
-
Molecular Weight 351.33
-
Formula C17H18N3NaO4
-
SMILES
N#C/C(C(O[Na])=O)=C\C1=C(OC(C)C)N=C2C(OC(C)C)=CC=CN21
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)