[CAS NO. 1345808-25-4] Arginaseinhibitor1
PRODUCTS SPECIFICATIONS [1345808-25-4]
DESCRIPTION [1345808-25-4]
Overview
| MDL | MFCD28167713 |
|---|---|
| Molecular Weight | 286.18 |
| Molecular Formula | C13H27BN2O4 |
| SMILES | O=C(O)[C@@](CCN1CCCCC1)(N)CCCCB(O)O |
4 Publications Citing Use of MCE
Summary
Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC 50 s 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 IC 50 s 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 IC 50 for Arginase inhibitor 1 is 8 μM in CHO Cells Over-Expressing hArgI [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 (t 1/2 ) 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 C max of 0.45 mg/L [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : ≥ 48 mg/mL ( 167.73 mM )
H 2 O : ≥ 30 mg/mL ( 104.83 mM )
* "≥" means soluble, but saturation unknown.
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 |
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1.
Add each solvent one by one: PBS
Solubility: 65 mg/mL (227.13 mM); Clear solution; Need ultrasonic
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2.
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3.
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
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.67 mg/mL (5.84 mM); Clear solution