SIRT5-IN-10
SIRT5-IN-10 is a competitive SIRT5 inhibitor. SIRT5-IN-10 improves renal function and reduces histopathological damage in septic acute kidney injury (AKI) mice. SIRT5-IN-10 can be used for the research of sepsis-associated AKI.
For research use only. We do not sell to patients.
- Formula: C27H30N8O7S
- Molecular Weight:610.64
-
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
|
SIRT5 |
SIRT5-IN-10 (compound 56) (0.03-600 μM; 2 h) potently inhibits recombinant human SIRT5 catalytic domain with an IC50 of 0.29 μM at 100 μM NAD+ and 0.79 μM at 400 μM NAD+[1].
SIRT5-IN-10 acts as a dual competitive inhibitor of recombinant human SIRT5, competing for binding with both the NAD+ cofactor and the P16 substrate[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | Cmax | Tmax | T1/2 | Vz | CL | AUC0-24 |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 1601.71 ng/mL·h | 417.39 ng/mL | 0.69 h | 2.75 h | 73560 mL/kg | 6330 mL/h/kg | 1487.85 ng·h/mL |
SIRT5-IN-10 (40 mg/kg; i.p.; two doses (1 h pre-LPS injection and 8 h post-LPS (HY-D1056) injection)) significantly protects against LPS-induced septic AKI in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J mice (male, 8 weeks old) with CLP-induced septic AKI[1]
-
Dosage:20; 40 mg/kg
-
Administration:i.p.; two doses (1 h pre-surgery and 8 h post-surgery)
-
Result:Reduced serum blood urea nitrogen (BUN) and serum creatinine (Scr) levels at 40 mg/kg dose.
Mitigated tubular dilation and damage via H&E staining and tubular injury scoring at 40 mg/kg dose.
Downregulated renal mRNA expression of injury markers Havcr1 (KIM-1) and Lcn2 (NGAL) at 40 mg/kg dose.
Exhibited renoprotective effects at both doses, with 40 mg/kg being more potent.
Showed no statistically significant differences in serum ALT, AST, Scr, or BUN levels between compound-treated mice and normal controls.
Caused no notable histopathological changes in heart, liver, lung, spleen, or testis tissues.
-
Animal Model:C57BL/6J mice (male, 8 weeks old) with LPS-induced septic AKI[1]
-
Dosage:40 mg/kg
-
Administration:i.p.; two doses (1 h pre-LPS injection and 8 h post-LPS injection)
-
Result:Attenuated LPS-induced elevations in serum Scr and BUN levels.
Downregulated renal mRNA expression of KIM-1 and NGAL.
Ameliorated histopathological renal damage.
Partially normalized aberrant renal succinylation profiles.
Suppressed pro-inflammatory JAK-STAT signaling by reducing renal mRNA expression of Il6, Jak1, Jak2, and Stat3.
Lowered plasma CRP levels.
Decreased renal mRNA levels of inflammatory mediators Il6, Mcp1, and Tnf-α.
Chemical Information
-
Molecular Weight 610.64
-
Formula C27H30N8O7S
-
SMILES
O=C(C1=C(N=C(N=C1)C2=CC=C(S2)C(C)=O)NCCCN/C(NCCC(O)=O)=C\[N+]([O-])=O)NC3=CC=CC(NC(C)=O)=C3
-
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)
SIRT5-IN-10 Related Classifications
HY-184000 Related Classifications
Powered by Bioz