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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
Description
IC50 & Target
[2]|
E-selectin 150 μg/mL (IC50) |
VCAM-1 115 μg/mL (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HUVEC | IC50 |
150 μg/mL
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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.
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8737744 |
| HUVEC | IC50 |
760 μg/mL
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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.
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8737744 |
| HUVEC | IC50 |
115 μg/mL
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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.
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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. Further protocols information, click here.
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Cell Line:human umbilical vein endothelial cells (HUVEC)
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Concentration:1 mg/mL
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Incubation Time:1 h pre-incubation
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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.
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Animal Model:BALB/c (7-week-old female, specific pathogen-free, septic shock model via intravenous LD100 LPS injection)[1]
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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)
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Administration:i.v.; single dose
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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
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CAS No. 133669-72-4
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Molecular Weight 351.33
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Formula C17H18N3NaO4
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SMILES
N#C/C(C(O[Na])=O)=C\C1=C(OC(C)C)N=C2C(OC(C)C)=CC=CN21
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sjc 13 Related Classifications
HY-187596 Related Classifications
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