2. Immunology/Inflammation
  3. VAP-1
  4. 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.

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VAP-1-IN-2

VAP-1-IN-2 Chemical Structure

CAS No. : 1279026-89-9

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VAP-1-IN-2 Related Antibodies

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Description

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[1][2].

In Vitro

VAP-1-IN-2 (Compound 1/17hd) potently inhibits recombinant human VAP-1 with an IC50 of 0.025 μM; it also potently inhibits recombinant rat VAP-1 with an IC50 of 0.015 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

VAP-1-IN-2 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-24 CLtotal T1/2 Vdss Cmax Bioavailability
Rat[2] 1 mg/kg i.v. 1920 ng·h/mL 8.69 mL/min/kg 1.39 h 0.386 L/kg / /
Rat[2] 1 mg/kg p.o. 334 ng·h/mL / 1.29 h / 113 ng/mL 17.4 %
In Vivo

VAP-1-IN-2 (0.3-1 mg/kg; p.o.; single administration) inhibits VAP-1 activity in rats[1][2].
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.

Animal Model: Sprague-Dawley (male)/Wistar (male)[1]
Dosage: 0.3 mg/kg/0.3 mg/kg; 1 mg/kg
Administration: p.o.; single dose
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).
Animal Model: Sprague Dawley (SD) (male, 6 weeks old; streptozotocin-induced diabetes)[2]
Dosage: 0.3 mg/kg; 1 mg/kg
Administration: p.o.; once daily; 4 weeks
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).
Molecular Weight

494.98

Formula

C25H27ClN6O3
CAS No.
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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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
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VAP-1-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VAP-1-IN-21279026-89-9VAP-1Vascular adhesion protein-1 (VAP-1)Semicarbazide-sensitive amine oxidase (SSAO)Amine oxidase copper-containing 3 (AOC3)VAP-1 inhibitorSprague-Dawley ratWistar ratdiabetesnephropathyInhibitorinhibitorinhibit

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