Vasopressin V2 receptor antagonist 1
Vasopressin V2 receptor antagonist 1 is a vasopressin V2 receptor (V2R) antagonist with a Ki value of 3.8 nM. Vasopressin V2 receptor antagonist 1 inhibits renal cyst formation in embryonic renal cyst models and mouse models. Vasopressin V2 receptor antagonist 1 can be used in research related to autosomal dominant polycystic kidney disease.
For research use only. We do not sell to patients.
- CAS No.: 2648650-50-2
- Formula: C33H37ClN4O4
- Molecular Weight:589.12
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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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
V2 Receptor 3.8 nM (Ki) |
In Vitro
Vasopressin V2 receptor antagonist 1 (Compound 4g) (2 h) competes for binding to SNAP-tagged V2R in HEK293 cells, with a Ki value of 3.8 nM; its residence time at V2R in HEK293 cells is 9 minutes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t |
|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | s.c. | 0.29 h | 0.14 h | 783 ng/mL | 450 ng·h/mL |
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 (Pkd1flox/flox;Ksp-Cre, neonatal, postnatal day 2, kidney-specific Pkd1 gene knockout)[1]
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Dosage:2 mg/kg
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Administration:s.c.; daily; 7 days
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Result:Reduced the relative kidney size (KW/BW ratio) compared to vehicle-treated mice.
Reduced renal cyst formation compared to vehicle-treated mice.
Chemical Information
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CAS No. 2648650-50-2
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Molecular Weight 589.12
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Formula C33H37ClN4O4
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SMILES
ClC1=CC2=C(C=C1)N(C(C3=C(C=C(C=C3)NC(C4=C(C=CC=C4)C)=O)C)=O)CCCC2NCCC(N5CCOCC5)=O
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Vasopressin V2 receptor antagonist 1 Related Classifications
HY-146272 Related Classifications
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Keywords
- Vasopressin V2 receptor antagonist 1
- 2648650-50-2
- Vasopressin Receptor
- SNAP-tagged V2R
- autosomal dominant polycystic kidney disease
- renal cyst development
- HEK293 cells
- vasopressin V2 receptor
- kidney-specific Pkd1 knockout mouse models
- early-onset ADPKD knockout mice
- ex vivo embryonic kidney cyst models
- Inhibitor
- inhibitor
- inhibit