VAP-1-IN-2
VAP-1-IN-2 is an orally active VAP-1 inhibitor with an IC50 value of 0.025 μM against human VAP-1 and 0.015 μM against rat VAP-1. VAP-1-IN-2 inhibits urinary protein excretion and the progression of proteinuria in diabetic rats. VAP-1-IN-2 inhibits VAP-1 activity in rats. VAP-1-IN-2 can be used in research related to diabetes and nephropathy.
For research use only. We do not sell to patients.
- CAS No.: 1279026-89-9
- Formula: C25H27ClN6O3
- Molecular Weight:494.98
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
VAP-1-IN-2 (0.3-1 mg/kg; p.o.; once daily; for 4 consecutive weeks) significantly inhibits the progression of proteinuria and plasma VAP-1 activity in streptozotocin (HY-13753)-induced diabetic rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male)/Wistar (male)[1]
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Dosage:0.3 mg/kg/0.3 mg/kg; 1 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited rat plasma VAP-1 activity by 92% at 1 hour post-dose.
Inhibited rat plasma VAP-1 activity by 74% at 6 hours post-dose.
Inhibited plasma VAP-1 activity by 64% at 1 hour post-dose and 62% at 6 hours post-dose (0.3 mg/kg).
Inhibited plasma VAP-1 activity by 96% at 1 hour post-dose and 93% at 6 hours post-dose (1 mg/kg).
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Animal Model:Sprague Dawley (SD) (male, 6 weeks old; streptozotocin-induced diabetes)[2]
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Dosage:0.3 mg/kg; 1 mg/kg
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Administration:p.o.; once daily; 4 weeks
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Result:Significantly inhibited the progression of proteinuria compared to the STZ control group (0.3 mg/kg and 1 mg/kg).
Significantly inhibited plasma VAP-1 activity in STZ-induced diabetic rats 24 hours after the final dose (0.3 mg/kg and 1 mg/kg).
Chemical Information
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CAS No. 1279026-89-9
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Molecular Weight 494.98
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Formula C25H27ClN6O3
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SMILES
O=C(O)C1=CC=C(C(Cl)=C1)N2CCN(C=3N=CC(=CN3)C4=CC=CC(=C4)CN(C(=O)CN)C)CC2
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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
[1]. Yamaki S, et al. Synthesis and structure activity relationships of carbamimidoylcarbamate derivatives as novel vascular adhesion protein-1 inhibitors. Bioorg Med Chem. 2017 Nov 1;25(21):6024-6038. [Content Brief]
[2]. Yamaki S, et al. Synthesis and pharmacological evaluation of glycine amide derivatives as novel vascular adhesion protein-1 inhibitors without CYP3A4 and CYP2C19 inhibition. Bioorg Med Chem. 2017 Aug 1;25(15):4110-4122. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VAP-1-IN-2 Related Classifications
HY-153506 Related Classifications
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