GV-001
GV-001 is a selective and orally active HDAC6 inhibitor with an IC50 of 1.18 nM against HDAC6. GV-001 selectively enhances α-tubulin acetylation, reduces sIL-6 and Collagen I levels, suppresses renal cyst growth, and upregulates PC1 expression. GV-001 can be used for the study of autosomal dominant polycystic kidney disease (ADPKD).
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- CAS. Nr.: 3082707-76-1
- Formel: C17H15N3O3
- Molecular Weight:309.32
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
HDAC6 1.18 nM (IC50) |
IL-6 |
Collagen I |
α-Tubulin |
In Vitro
GV-001 (6a) (2 h) potently and selectively inhibits recombinant human HDAC6 with an IC50 of 1.18 nM, showing 1991-fold selectivity over HDAC1 and 247-fold selectivity over HDAC8[1].
GV-001 (0.00152-30 μM; 16 h) selectively upregulates acetylated α-tubulin in HepG2 cells with an IC50 of 0.19 μM, showing 24-fold selectivity over acetylated histone H3 (IC50 = 4.46 μM)[1].
GV-001 (370 nM-10 μM; 48 h) modulates key inflammatory, fibrotic, and tissue remodeling biomarkers in human primary cell-based MyoF and REMyoF fibrosis models at noncytotoxic concentrations[1].
GV-001 (0.1-100 μM; 14 days) potently inhibits cyst formation in a 3D in vitro human ADPKD model, with IC50 values of 0.42 μM for cyst viability, 2.22 μM for cyst number, 0.92 μM for total cyst area, and 2.38 μM for average cyst size, without cytotoxicity at active concentrations[1].
GV-001 (0.001-100 μM; 12 days) potently reduces established cyst growth in a 3D in vitro human ADPKD model, with IC50 values of 8.36 μM for cyst viability, 13.3 μM for cyst number, 10.8 μM for total cyst area, and 18.5 μM for average cyst size[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0.00152, 0.00457, 0.0137, 0.0412, 0.123, 0.37, 1.11, 3.33, 10, 30 μM
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Incubation Time:16 h
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Result:Induced dose-dependent upregulation of acetylated α-tubulin with an IC50 of 0.19 μM.
Upregulated acetylated histone H3 with an IC50 of 4.46 μM.
Resulted in a 24-fold selectivity for α-tubulin acetylation over histone H3 acetylation.
Parmacokinetics
| Species | Dose | Route | C0 | T1/2 | AUC0-t | AUC0-∞ | Cmax | Tmax | Bioavailability | T1/2 (Plasma) | AUC0-∞ (Plasma) |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 559 ng/mL | 0.173 h | 98.5 ng·h/mL | 99.8 ng·h/mL | / | / | / | / | / |
| Rat[1] | 30 mg/kg | p.o. | / | 2.94 h | 1018 ng·h/mL | 1087 ng·h/mL | 480 ng/mL | 0.250 h | 36 % | / | / |
| Rat[1] | 30 mg/kg | p.o. | / | / | / | / | / | / | / | 3.90 h | 997 ng·h/mL |
| Mice[1] | 1 mg/kg | i.v. | 1222 ng/mL | 0.200 h | 184 ng·h/mL | 184 ng·h/mL | / | / | / | / | / |
| Mice[1] | 30 mg/kg | p.o. | / | 2.49 h | 643 ng·h/mL | 694 ng·h/mL | 635 ng/mL | 0.250 h | 13 % | / | / |
| Mice[1] | 60 mg/kg | p.o. | / | 5.70 h | 1408 ng·h/mL | 2561 ng·h/mL | 834 ng/mL | 0.250 h | 13 % | / | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 Tg(Ubi-emGFP Pkd1miRNA)1SJi/Narl transgenic mice (males and females, 14 days old at study start, stable Pkd1 knockdown via miRNA expression)[1]
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Dosage:60 mg/kg; 120 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Reduced the average kidney-to-body weight ratio to 3.4% and reduced the cystic index to 22.7%.
Reduced the average kidney-to-body weight ratio to 3.2% and reduced the cystic index to 20.7%.
Increased PC1 positive area.
Chemical Information
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CAS. Nr. 3082707-76-1
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Molecular Weight 309.32
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Formel C17H15N3O3
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SMILES
O=C(NO)C1=CC=C(CC(N2C)=NC3=C(C=CC=C3)C2=O)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
GV-001 Related Classifications
HY-182904 Related Classifications
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