1. Immunology/Inflammation
    Metabolic Enzyme/Protease
  2. Arginase
  3. Arginase inhibitor 1

Arginase inhibitor 1 

Cat. No.: HY-15775 Purity: >98.0% ee.: 98.00%
Handling Instructions

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.

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

Arginase inhibitor 1 Chemical Structure

Arginase inhibitor 1 Chemical Structure

CAS No. : 1345808-25-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 317 In-stock
Estimated Time of Arrival: December 31
5 mg USD 288 In-stock
Estimated Time of Arrival: December 31
10 mg USD 504 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3120 In-stock
Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

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Description

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.

IC50 & Target

IC50: 223 nM (arginases I), 509 nM (arginases II)[1]

In Vitro

Arginase inhibitor 1inhibits human arginases I and II with IC50s of 223±22.3 and 509±85.1 nM, respectively, and is active in a recombinant cellular assay overexpressing human arginase I (CHO cells). Arginase inhibitor 1 is a novel second generation arginase inhibitor with significant activity in a rat model of myocardial ischemia/reperfusion injury (MI/RI). Arginase inhibitor 1 is potent against hARG I in both in vitro enzyme and cellular assays. The IC50 for Arginase inhibitor 1 is 8 μM in CHO Cells Over-Expressing hArgI[1].

In Vivo

A pharmacokinetic evaluation of Arginase inhibitor 1 is conducted after intravenous (i.v.) and oral (p.o.) dosing in male Sprague-Dawley rats (n=3 per dose route). Arginase inhibitor 1 is formulated in 0.9% saline and administered intravenously at 10 mg/kg by bolus through a preimplanted cannula at a dosing volume of 1 mL/kg, and orally at 10 mg/kg via gavage at a dosing volume of 2 mL/kg. Following i.v. dosing with 10 mg/kg in fasted animals, Arginase inhibitor 1has a terminal elimination half-life (t1/2) of 3.3 h with a volume of distribution and total body clearance of 1.86 L/kg and 7.89 mL/min/kg, respectively. The oral bioavailability of Arginase inhibitor 1 (10 mg/kg, p.o.) is 28% with a Cmax of 0.45 mg/L[1].

Molecular Weight

286.18

Formula

C₁₃H₂₇BN₂O₄

CAS No.

1345808-25-4

SMILES

O=C(O)[[email protected]@](CCN1CCCCC1)(N)CCCCB(O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 48 mg/mL (167.73 mM)

H2O : ≥ 30 mg/mL (104.83 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4943 mL 17.4715 mL 34.9430 mL
5 mM 0.6989 mL 3.4943 mL 6.9886 mL
10 mM 0.3494 mL 1.7472 mL 3.4943 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (5.84 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (5.84 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (5.84 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats[1]
Single dose pharmacokinetics are evaluated in male Sprague-Dawley rats by intravenous bolus (i.v.) and oral (p.o.) dosing. Three rats are evaluated per dose group. Arginase inhibitor 1 is freshly formulated in 0.9% saline prior to dosing, at 10 mg/mL for i.v. dosing at a dose volume of 1 mL/kg animal body weight, and at 5 mg/mL for p.o. dosing at a dose volume of 2 mL/kg. Animals are fasted overnight prior to dosing, with water given ad libitum. Arginase inhibitor 1 is administered i.v. through a preimplanted cannula or orally by gavage. Food is reintroduced to animals 4 h following dosing. Blood samples are collected through preimplanted cannulae (dual cannulated animals used for i.v. dosing; blood collection separate from dosing cannula) at 0.25 mL per draw, followed by volume replacement with 0.9% saline. Samples are collected at predose 0.083 (i.v. only), 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h following dosing. Blood samples are maintained on ice and centrifuged at 10 000g to obtain plasma. Plasma is frozen at -20 °C prior to analysis. Analysis is performed by LC/MS/MS. Pharmacokinetic evaluation is performed using standard noncompartmental analyses in Phoenix WinNonlin software.

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

References

Purity: >98.0% ee.: 98.00%

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Arginase inhibitor 1Arginase inhibitor1Arginase inhibitor-1ArginaseInhibitorinhibitorinhibit

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Arginase inhibitor 1
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