2. Immunology/Inflammation
  3. VAP-1
  4. PXS-4681A

PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects.

For research use only. We do not sell to patients.

PXS-4681A Chemical Structure

PXS-4681A Chemical Structure

CAS No. : 1478364-87-2

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Based on 1 publication(s) in Google Scholar

PXS-4681A Related Antibodies

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Description

PXS-4681A is a potent, selective, irreversible and orally active semicarbazide-sensitive amine oxidase (SSAO; VAP-1) inhibitor with a Ki of 37 nM. PXS-4681A shows highly selectivity over related amine oxidases, ion channels, and seven-transmembrane domain receptors. PXS-4681A has anti-inflammatory effects[1].

IC50 & Target

Ki: 37 nM (SSAO)[1]
In Vitro

PXS-4681A is an inhibitor of SSAO/VAP-1 in human, rat, mouse, rabbit, and dog species with IC50 values of 3 nM, 3 nM, 2 nM, 9 nM and 3nM, respectively[1].

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

PXS-4681A Related Antibodies
In Vivo

PXS-4681A (2 mg/kg; PO; single dose) attenuates neutrophil migration, tumor necrosis factor-α, and interleukin-6 levels in mouse models of lung inflammation and localized inflammation[1].
In rats, PXS-4681A is well absorbed with good bioavailability and oral half-life at the 10 mg/kg i.v. dose and the 20 mg/kg PO dose. Similarly, in BALB/C mice, PXS-4681A is well absorbed with good bioavailability and oral half-life at 2 mg/kg in both intravenous and oral studies[1].

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

Animal Model: Carrageenan-induced skin inflammation mice[1]
Dosage: 2 mg/kg
Administration: oral administration; single dose
Result: Reduced local inflammation, causing a significant reduction in exudate volume by 25%.
Molecular Weight

296.75

Formula

C10H14ClFN2O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(OC/C(CN)=C\F)C=C1)(N)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (842.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3698 mL 16.8492 mL 33.6984 mL
5 mM 0.6740 mL 3.3698 mL 6.7397 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3698 mL 16.8492 mL 33.6984 mL 84.2460 mL
5 mM 0.6740 mL 3.3698 mL 6.7397 mL 16.8492 mL
10 mM 0.3370 mL 1.6849 mL 3.3698 mL 8.4246 mL
15 mM 0.2247 mL 1.1233 mL 2.2466 mL 5.6164 mL
20 mM 0.1685 mL 0.8425 mL 1.6849 mL 4.2123 mL
25 mM 0.1348 mL 0.6740 mL 1.3479 mL 3.3698 mL
30 mM 0.1123 mL 0.5616 mL 1.1233 mL 2.8082 mL
40 mM 0.0842 mL 0.4212 mL 0.8425 mL 2.1061 mL
50 mM 0.0674 mL 0.3370 mL 0.6740 mL 1.6849 mL
60 mM 0.0562 mL 0.2808 mL 0.5616 mL 1.4041 mL
80 mM 0.0421 mL 0.2106 mL 0.4212 mL 1.0531 mL
100 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8425 mL
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PXS-4681A Related Classifications

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:

PXS-4681A1478364-87-2VAP-1Vascular adhesion protein-1 (VAP-1)Semicarbazide-sensitive amine oxidase (SSAO)Amine oxidase copper-containing 3 (AOC3)anti-inflammatorySSAOoralInhibitorinhibitorinhibit

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