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  4. Inosine

Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors.

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Inosine Chemical Structure

Inosine Chemical Structure

CAS No. : 58-63-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 28 In-stock
Solution
10 mM * 1 mL in DMSO USD 28 In-stock
Solid
500 mg USD 25 In-stock
25 g USD 50 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Inosine:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors[1][2][3].

IC50 & Target[1]

Human Endogenous Metabolite

 

A1AR

 

A2AR

 

Cellular Effect
Cell Line Type Value Description References
C6 IC50
> 250 μM
Compound: Inosine
Cytotoxicity against rat C6 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
Cytotoxicity against rat C6 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
10.1039/C3MD00159H
DU-145 IC50
> 250 μM
Compound: Inosine
Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
10.1039/C3MD00159H
HaCaT IC50
> 250 μM
Compound: Inosine
Cytotoxicity against human HaCaT cells assessed as inhibition of cell viability after 48 hrs by MTT assay
Cytotoxicity against human HaCaT cells assessed as inhibition of cell viability after 48 hrs by MTT assay
10.1039/C3MD00159H
L6 IC50
> 250 μM
Compound: Inosine
Cytotoxicity against rat L6 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
Cytotoxicity against rat L6 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
10.1039/C3MD00159H
MCF7 IC50
> 250 μM
Compound: Inosine
Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by MTT assay
10.1039/C3MD00159H
Vero IC50
0.23 nM
Compound: Inosine
Anti-Herpes simplex virus type-1 activity in vero cells using plaque inhibition assay
Anti-Herpes simplex virus type-1 activity in vero cells using plaque inhibition assay
[PMID: 10464017]
In Vitro

Inosine dose-dependently stimulates cAMP production mediated through the A2AR[2].
Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation[2].
Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes[3].

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

In Vivo

Inosine can induce hyperuricemia[5].

Induction of Hyperuricemia[5]
Background
Hyperuricaemia (HUA) occurs because of purine metabolism aberrations and is typically characterized by increased uric acid formation or reduced uric acid excretion. Inosineis a precursor of purine metabolism. Purine nucleoside phosphorylase (PNP) and xanthine oxidase (XO) catalyse the conversion of inosine [6]. Inosinecan further catalyzed hypoxanthine, xanthine and uric acid (UA)[7].
Specific Mmodeling Methods
Mice: Alb-CreERT2;Glut9lox/lox (LG9KO) &bulll; 6-week-old
Administration: 4 g/kg • ig • one time daily at 9: 00-10: 00 A.M. for 3 days
Note
(1)Mice was gavaged one time daily at 9:00–10:00 A.M. for 3 days (days 0, 1, and 2) with 4 g/kg inosine (500 mg/ml in 0.5% carboxymethylcellulose aqueous suspension) and euthanized 24 h after the last inosine gavage (day 3).
(2)Blood was collected from tail bleeds for plasma urate and creatinine measurements before the inosine treatment and 2 h, 6 h after the first gavage, and 24 h after the last gavage before the animals were euthanized.
(3)Six weeks after inosine gavage, plasma urate and creatinine had normalized.
Inosine gavage combines with HFD to cause acute renal failure in LG9KO mice.
Modeling Indicators
Molecular changes: Inosine elevates plasma urate levels in LG9KO mice. In LG9KO mice fed chow, uricemia transiently rose 2 and 6 h after the first gavage and returned to their basal level 24 h after the last gavage (day 3). In contrast, in HFD-fed LG9KO mice, inosine gavage induced a much higher hyperuricemia at day 3
Tissue changes: leads to tubular urate and uric acid crystal formation.
Correlated Product(s): Potassium oxonate (HY-17511)
Opposite Product(s): /

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

Animal Model: Male/female C57BL/6 mice[2]
Dosage: 1 mg/kg, 10 mg/kg, 100 mg/kg
Administration: Intraperitoneal injection, 20 min before formalin treatment
Result: Reduced flinching behaviour induced by formalin (2 %; 20 μL; intraplantar injection).
Clinical Trial
Molecular Weight

268.23

Formula

C10H12N4O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N2C=NC3=C2N=CNC3=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 100 mg/mL (372.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 10 mg/mL (37.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.7282 mL 18.6408 mL 37.2816 mL
5 mM 0.7456 mL 3.7282 mL 7.4563 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.5 mg/mL (9.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (9.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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: 15.56 mg/mL (58.01 mM); Clear solution; Need ultrasonic

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.67%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.7282 mL 18.6408 mL 37.2816 mL 93.2039 mL
5 mM 0.7456 mL 3.7282 mL 7.4563 mL 18.6408 mL
10 mM 0.3728 mL 1.8641 mL 3.7282 mL 9.3204 mL
15 mM 0.2485 mL 1.2427 mL 2.4854 mL 6.2136 mL
20 mM 0.1864 mL 0.9320 mL 1.8641 mL 4.6602 mL
25 mM 0.1491 mL 0.7456 mL 1.4913 mL 3.7282 mL
30 mM 0.1243 mL 0.6214 mL 1.2427 mL 3.1068 mL
DMSO 40 mM 0.0932 mL 0.4660 mL 0.9320 mL 2.3301 mL
50 mM 0.0746 mL 0.3728 mL 0.7456 mL 1.8641 mL
60 mM 0.0621 mL 0.3107 mL 0.6214 mL 1.5534 mL
80 mM 0.0466 mL 0.2330 mL 0.4660 mL 1.1650 mL
100 mM 0.0373 mL 0.1864 mL 0.3728 mL 0.9320 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.

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Inosine
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