Keap1-Nrf2-IN-11
Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research.
For research use only. We do not sell to patients.
- CAS No.: 2796292-75-4
- Formula: C36H43N7O8S2
- Molecular Weight:765.90
-
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
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Peritoneal macrophage | CC50 |
>100 μM
Compound: 6k
|
Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by Cell Titer-Blue assay
Cytotoxicity against mouse peritoneal macrophages assessed as reduction in cell viability measured after 24 hrs by Cell Titer-Blue assay
|
[PMID: 35687391] |
| Peritoneal macrophage | EC50 |
0.97 μM
Compound: 6k
|
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as suppression of NO level pretreated with LPS followed by compound addition and measured after 24 hrs by Griess reagent based assay
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as suppression of NO level pretreated with LPS followed by compound addition and measured after 24 hrs by Griess reagent based assay
|
[PMID: 35687391] |
| Peritoneal macrophage | EC50 |
1.14 μM
Compound: 6k
|
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as inhibition of TNF alpha level after 4 hrs by ELISA method
Antiinflammatory activity against LPS-induced mouse peritoneal macrophage assessed as inhibition of TNF alpha level after 4 hrs by ELISA method
|
[PMID: 35687391] |
Keap1-Nrf2-IN-11 (compound 6k) (10 μΜ) suppresses the production of ROS and NO and inhibits the concentration of proinflammatory cytokine TNF-α in LPS-induced murine peritoneal macrophage model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Keap1-Nrf2-IN-11 (compound 6k) (5 mg/kg; i.v.; SD rats) has the half time (T1/2), the clearance rate (CL) and apparent distribution volume (V) were 4.31 h, 5.57 mL/min/kg and 959 L/kg, respectively[1].
Keap1-Nrf2-IN-11 (compound 6k) (5 mg/kg; i.p.; ALI mouse model) has the half time (T1/2), maximum plasma concentration (Cmax), area under curve (AUC) and oral bioavailability (F) were 10.92 h, 707 ng/mL, 3702 ng•h/mL and 19.86%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:ALI mouse model[1]
-
Dosage:5, 10 and 20 mg/kg
-
Administration:Intraperitoneal injection; 30 mins.
-
Result:Had lower TNF-α, IL-1β and IL-6 levels in BALF in a dose-dependent manner.
-
Animal Model:ALI mouse model[1]
-
Dosage:5, 10 and 20 mg/kg
-
Administration:Intraperitoneal injection; 30 mins.
-
Result:Induced the Nrf2 nuclear accumulation in lung tissue cells by decreasing the cytosolic Nrf2 and increasing the nuclear Nrf2 in a dose−response manner.
-
Animal Model:SD rats[1]
-
Dosage:5 and 20 mg/kg
-
Administration:Intraperitoneal injection and oral gavage
-
Result:
1.19 Administration i.g. (20 mg/kg) i.v. (5 mg/kg) Tmax (h) 1.38 0.72 Tmax (h) 10.92 4.31 Cmax (ng/mL) 707.62 2631.69 AUC0-24 (ng·h/mL) 3061.55 4561.21 AUC0-∞ (ng·h/mL)CL (mL/min/kg) 3702.22 4799.24 CL (L/h/kg) 6503.05 5.57 V (L/kg) 114127.5 959.54 MRT0-24 (h) 6.71 4.64 MRT0-∞ (h) 13.97 5.94 F % 19.86
Chemical Information
-
CAS No. 2796292-75-4
-
Molecular Weight 765.90
-
Formula C36H43N7O8S2
-
SMILES
O=S(N(C1=C2C(C=CC=C2)=C(C=C1)N(S(=O)(C3=CC=C(C=C3)NC(CCN4CCN(CC4)CC)=O)=O)CC(N)=O)CC(N)=O)(C5=CC=C(C=C5)OC)=O
-
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)
Keap1-Nrf2-IN-11 Related Classifications
HY-147924 Related Classifications
Powered by Bioz