NOD1 antagonist-3
NOD1 antagonist-3 is an orally active selective NOD1 antagonist with IC50 values of 0.35 nM and 19 nM for hNOD1 and mNOD1, respectively. NOD1 antagonist-3 blocks the activation of the NOD1 signaling pathway by antagonizing the NOD1 receptor, thereby inhibiting the phosphorylation activation of the downstream RIP2, NF-κB (p65), and MAPK (p38, JNK) signaling cascades, and ultimately reducing the release of pro-inflammatory cytokines and alleviating inflammatory injury of pancreatic tissue. NOD1 antagonist-3 can be used for research on acute pancreatitis.
For research use only. We do not sell to patients.
- Formula: C19H9ClF5N5O3S3
- Molecular Weight:581.95
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
hNOD1 |
mNOD1 |
JNK |
RIPK2 |
p65 |
p38 |
In Vitro
NOD1 antagonist-3 (10-500 nM; 45 min pretreatment followed by 30-60 min stimulation) dose-dependently inhibits C12-iE-DAP (HY-P5524)-induced phosphorylation of RIP2, p65, p38, and JNK in THP-1, BMDM, H6C7, and 266-6 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:THP-1, BMDM, H6C7, and 266-6 cells
-
Concentration:10, 100, 500 nM
-
Incubation Time:45 min pretreatment, followed by 30 min (for THP-1 and BMDMs) or 1 h (for H6C7 and 266-6) stimulation with C12-iE-DAP
-
Result:Dose-dependently suppressed the agonist-induced phosphorylation of downstream key signaling proteins (RIP2, p65, p38, JNK).
-
Cell Line:THP-1 and BMDMs
-
Concentration:10, 100 nM
-
Incubation Time:45 min pretreatment, followed by 2 h stimulation with C12-iE-DAP
-
Result:Profoundly suppressed the NOD1-driven transcriptional upregulation of pro-inflammatory cytokines, nearly abolishing IL-6 transcription and substantially downregulating TNF-α expression.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (male, 6-8 weeks old) were i.p. with 100 ng/kg of the NOD1-specific agonist C12-iE-DAP[1]
-
Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
-
Administration:p.o.; single dose; administered 15 min prior to C12-iE-DAP injection, and euthanized 2 h post-induction for blood collection.
-
Result:Dose-dependently reduced serum KC chemokine concentrations, significantly suppressing the systemic inflammatory response in vivo.
Chemical Information
-
Molecular Weight 581.95
-
Formula C19H9ClF5N5O3S3
-
SMILES
O=C1C2=C(NC(N1C3=CC(NS(=O)(C4=C(C=CC=C4F)F)=O)=C(C=C3)Cl)=S)N=C(N=C2)SC(F)(F)F
-
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)
NOD1 antagonist-3 Related Classifications
HY-191406 Related Classifications
Powered by Bioz