Arginase inhibitor 1

Name: Arginase inhibitor 1
Brand: MedChemExpress
SKU: HY-15775
Rating: 5.0 (5 reviews)

Cat. No.: HY-15775 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1345808-25-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 349	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 349	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 317	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 554	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2112	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3432	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE Arginase inhibitor 1

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	3 μM Compound: 9	Inhibition of human arginase 1 transfected in CHO cells assessed as inhibition of urea formation after 24 hrs by spectrophotometric analysis Inhibition of human arginase 1 transfected in CHO cells assessed as inhibition of urea formation after 24 hrs by spectrophotometric analysis	[PMID: 23472952]

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]

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

In Vivo

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].

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

Molecular Weight

286.18

Formula

C₁₃H₂₇BN₂O₄

CAS No.

1345808-25-4

Appearance

Solid

Color

White to gray

SMILES

O=C(O)[C@@](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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 65 mg/mL (227.13 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (245 KB) HNMR (195 KB)

Handling Instructions (2659 KB)

References

[1]. Van Zandt MC, et al. Discovery of (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid and congeners as highly potentinhibitors of human arginases I and II for treatment of myocardial reperfusion injury. J Med Chem. 2013 Mar 28;56(6):2568-80. [Content Brief]

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

[1]. Van Zandt MC, et al. Discovery of (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid and congeners as highly potentinhibitors of human arginases I and II for treatment of myocardial reperfusion injury. J Med Chem. 2013 Mar 28;56(6):2568-80. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	3.4943 mL	17.4715 mL	34.9430 mL	87.3576 mL
	5 mM	0.6989 mL	3.4943 mL	6.9886 mL	17.4715 mL
	10 mM	0.3494 mL	1.7472 mL	3.4943 mL	8.7358 mL
	15 mM	0.2330 mL	1.1648 mL	2.3295 mL	5.8238 mL
	20 mM	0.1747 mL	0.8736 mL	1.7472 mL	4.3679 mL
	25 mM	0.1398 mL	0.6989 mL	1.3977 mL	3.4943 mL
	30 mM	0.1165 mL	0.5824 mL	1.1648 mL	2.9119 mL
	40 mM	0.0874 mL	0.4368 mL	0.8736 mL	2.1839 mL
	50 mM	0.0699 mL	0.3494 mL	0.6989 mL	1.7472 mL
	60 mM	0.0582 mL	0.2912 mL	0.5824 mL	1.4560 mL
	80 mM	0.0437 mL	0.2184 mL	0.4368 mL	1.0920 mL
	100 mM	0.0349 mL	0.1747 mL	0.3494 mL	0.8736 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.