Cat. No.: HY-B0219

Allopurinol

12 Cited Publications

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Based on 12 publication(s) in Google Scholar

Allopurinol is a potent and orally active xanthine oxidase inhibitor with an IC₅₀ value of 0.2-50 μM. Allopurinol can be used in the research of hyperuricemia and gout. Allopurinol decreases the expression of HIF-1α and HIF-2α protein. Allopurinol shows anti-depressant and anti-nociception activity. Anti-leishmanial effect.

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Pureté: 99.96%
CAS No.: 315-30-0
Formule: C₅H₄N₄O
Masse moléculaire:136.11

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Allopurinol Chemical Structure

CAS No.: 315-30-0

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (12)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
L02	CC₅₀	6.842 μM Compound: Allopurinol	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 35902063]
MRC5	CC₅₀	>64 μM Compound: Allopurinol	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 3 days by resazurin dye based fluorescence analysis Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 3 days by resazurin dye based fluorescence analysis	[PMID: 35533570]
Peritoneal macrophage	CC₅₀	>64 μM Compound: 1	Cytotoxicity against Swiss mouse peritoneal macrophages assessed as cell detachment, lysis and granulation measured after 5 days by microscopic analysis Cytotoxicity against Swiss mouse peritoneal macrophages assessed as cell detachment, lysis and granulation measured after 5 days by microscopic analysis	[PMID: 33784107]
Peritoneal macrophage	CC₅₀	>64 μM Compound: Allopurinol	Cytotoxicity against Swiss mouse peritoneal macrophages assessed as reduction in cell viability measured after 5 days by microscopic analysis Cytotoxicity against Swiss mouse peritoneal macrophages assessed as reduction in cell viability measured after 5 days by microscopic analysis	[PMID: 35533570]
Vero	CC₅₀	428 μM Compound: R8	Cytotoxicity against African green monkey Vero cells incubated for 24 hrs by neutral red uptake assay Cytotoxicity against African green monkey Vero cells incubated for 24 hrs by neutral red uptake assay	[PMID: 27933947]
Vero	IC₅₀	23.9 μM Compound: R8	Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by neutral red uptake assay Inhibition of Shigella dysenteriae type 1 Shiga toxin A subunit in African green monkey Vero cells assessed as inhibition of Stx-induced cytotoxicity pre-treated with compound for 1 hr followed by Stx exposure for 24 hrs by neutral red uptake assay	[PMID: 27933947]
Vero	IC₅₀	9.62 μM Compound: 1, allop, allopurinol	Antimicrobial activity against Trypanosoma cruzi RA amastigotes infected in African green monkey Vero cells assessed as growth inhibition after 72 hrs by Giemsa staining-based light microscopy Antimicrobial activity against Trypanosoma cruzi RA amastigotes infected in African green monkey Vero cells assessed as growth inhibition after 72 hrs by Giemsa staining-based light microscopy	[PMID: 24090917]

In Vitro

Allopurinol (0, 10, 100, 1000 μg/ml; 17 h) decreases the expression of HIF-1α and HIF-2α protein in HFF and HUVEC cells^[5].
Allopurinol (0, 10, 100, 1000 μg/ml; 24 h) reduces angiogenesis traits of HUVEC cells^[5].

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

Western Blot Analysis^[5]

Cell Line:

HFF, HUVEC cells
Concentration:

0, 10, 100, 1000 µg/ml
Incubation Time:

17 h
Result:

Reduced HIF-1α and HIF-2α protein expression in a dose dependent manner.

In Vivo

Allopurinol (39 mg/kg; p.o.; daily for 21 successive days) shows anti-depressant activity in mouse^[3].
Allopurinol (10-400 mg/kg; i.p.) induces anti-nociception activity in mouse^[4].

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

Animal Model:

20-30 g, male Swiss Albino mice^[3]
Dosage:

39 mg/kg
Administration:

P.o.; daily for 21 successive days
Result:

Reduced the immobility time in the FST with the immobility time of 129.8±10.5 s.

Animal Model:

30-40 g, male adult Swiss albino mice^[4]
Dosage:

10, 50, 100, 200, 400 mg/kg
Administration:

I.p.
Result:

Produced dose-dependent anti-nociception in the tail-flick, hot-plate.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 315-30-0
Appearance Solid
Masse moléculaire 136.11
Formule C₅H₄N₄O
Color White to off-white
SMILES

O=C1C2=C(NN=C2)N=CN1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (12)

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Adv Sci (Weinh)

Integrated Microbiome and Metabolome Analysis Reveals Hypothalamic-Comorbidities Related Signatures in Craniopharyngioma. [Abstract]

2024 Sep 3:e2400684. PMID: 39225628

Allopurinol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Sep 3:e2400684. [Abstract]

Quantitative analyses of histopathological results reveal a notable increase in collagen volume fraction (9.95 ± 0.50) and oil red area fraction (10.06 ± 0.64) in CP mice treated with WD + Hx, meanwhile NAC (collagen volume fraction: 5.29 ± 0.60; oil red area fraction: 0.08 ± 0.01) and Allopurinol (Allo, 2 g/L in the drinking water and a Western diet for 8 weeks) treatment (collagen volume fraction: 4.63 ± 0.36; oil red area fraction: 0.06 ± 0.001) induced remarkable alleviation in parameters above.

Allopurinol purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Sep 3:e2400684. [Abstract]

In the target organs (liver and brain cortex), Hx treatment suppressed the relative mRNA expression of critical enzymes in purine metabolism (HPRT, XOR, and PNP) as well as crucial players in anti‐oxidative system (Nrf2, SOD‐1, and CAT), meanwhile, NAC and Allopurinol (Allo, 2 g/L in the drinking water and a Western diet for 8 weeks) treatment induced significant upregulation in relative expression of these genes.
Cell Rep Med

The SGLT2 inhibitor dapagliflozin ameliorates renal fibrosis in hyperuricemic nephropathy. [Abstract]

2024 Aug 20;5(8):101690. PMID: 39168099
Mol Med

JAK2/STAT3/HMGCS2 signaling aggravates mitochondrial dysfunction and oxidative stress in hyperuricemia-induced cardiac dysfunction. [Abstract]

2025 May 13;31(1):184. PMID: 40361044

Allopurinol purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 13;31(1):184. [Abstract]

Allopurinol (10 mg/kg/day; oral gavage; once daily for 4 weeks) can significantly reduce the elevated IL-6 levels in the hearts of hyperuricemic mice.

Allopurinol purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 13;31(1):184. [Abstract]

Allopurinol (10 mg/kg/day; oral gavage; once daily for 4 weeks) effectively reduced the phosphorylation of JAK2 and STAT3 and decreased the expression of HMGCS2 protein in the hearts of hyperuricemic mice.

Allopurinol purchased from MedChemExpress. Usage Cited in: Mol Med. 2025 May 13;31(1):184. [Abstract]

Representative transmission electron microscopy images of mitochondria in cardiomyocytes. Scale bar: 500 nm. Electron microscopy revealed severe mitochondrial damage in cardiomyocytes of hyperuricemic mice, which was normalized by treatment with Allopurinol (10 mg/kg/day; oral gavage; once daily for 4 weeks).
Drug Deliv Transl Res

Leveraging quantum chemical properties in transfer learning for predicting blood-brain barrier permeability of drugs. [Abstract]

2025 Oct 29. PMID: 41160380
J Ethnopharmacol

Polysaccharide extracted from Phellinus igniarius attenuated hyperuricemia by modulating bile acid metabolism and inhibiting uric acid synthesis in adenine/potassium oxonate-treated mice. [Abstract]

2025 Jan 19:119365. PMID: 39837359
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Commun Biol

mTOR contributes to endothelium-dependent vasorelaxation by promoting eNOS expression and preventing eNOS uncoupling. [Abstract]

2022 Jul 22;5(1):726. PMID: 35869262
Pharmaceuticals (Basel)

Notopterol Ameliorates Hyperuricemia-Induced Cardiac Dysfunction in Mice. [Abstract]

2023 Feb 27;16(3):361. PMID: 36986461
Int J Mol Sci

Ampelopsis japonica Extract Exhibited Significant Uric Acid-Lowering Effect by Downregulating URAT1/GLUT9 and Alleviates Inflammation Through TLR4/NF- κ B Pathway. [Abstract]

2025 Sep 16;26(18):8999. PMID: 41009565
J Biol Chem

Type 2 diabetic mice enter a state of spontaneous hibernation-like suspended animation following accumulation of uric acid. [Abstract]

2021 Oct;297(4):101166. PMID: 34487763
Cytokine

Qinling liquid ameliorates renal immune inflammatory damage via activating autophagy through AMPK/Stat3 pathway in uric acid nephropathy. [Abstract]

2023 Mar:163:156120. PMID: 36630870
Biomed Pharmacother

Aqueous extract of Phellinus igniarius ameliorates hyperuricemia and renal injury in adenine/potassium oxonate-treated mice. [Abstract]

2024 Jun 15:177:116859. PMID: 38879892

Allopurinol purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Jun 15:177:116859. [Abstract]

Allopurinol (5 mg/kg; p.o.; single dose) significantly reduces the mRNA levels of XOD in HUA mice.

Solvant et solubilité

In Vitro:

DMSO : 14 mg/mL (102.85 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (7.35 mM; ultrasonic and adjust pH to 11 with NaOH)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

7.3468 mL

36.7339 mL

73.4678 mL

5 mM

1.4694 mL

7.3468 mL

14.6936 mL

10 mM

0.7347 mL

3.6734 mL

7.3468 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 3.33 mg/mL (24.46 mM); Clear solution

This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 3.33 mg/mL (24.46 mM); Clear solution

This protocol yields a clear solution of ≥ 3.33 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 (33.3 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

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

Solubility: ≥ 0.61 mg/mL (4.48 mM); Clear solution

This protocol yields a clear solution of ≥ 0.61 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.1 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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OR (2659 KB)
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Instruction de manipulation (2659 KB)

Références

[1]. Pacher P, et al. Therapeutic effects of xanthine oxidase inhibitors: renaissance half a century after the discovery of allopurinol. Pharmacol Rev. 2006 Mar;58(1):87-114. [Content Brief]

[2]. Pfaller MA, et al. Antileishmanial effect of allopurinol. Antimicrob Agents Chemother. 1974;5(5):469-472. [Content Brief]

[3]. Karve AV, et al. Evaluation of effect of allopurinol and febuxostat in behavioral model of depression in mice. Indian J Pharmacol. 2013 May-Jun;45(3):244-7. [Content Brief]

[4]. Schmidt AP, et al. Anti-nociceptive properties of the xanthine oxidase inhibitor allopurinol in mice: role of A1 adenosine receptors. Br J Pharmacol. 2009 Jan;156(1):163-72. [Content Brief]

[5]. Sun Y, et al. Dose-dependent effects of allopurinol on human foreskin fibroblast cells and human umbilical vein endothelial cells under hypoxia. PLoS One. 2015 Apr 1;10(4):e0123649. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	7.3468 mL	36.7339 mL	73.4678 mL	183.6696 mL
H₂O / DMSO	5 mM	1.4694 mL	7.3468 mL	14.6936 mL	36.7339 mL
DMSO	10 mM	0.7347 mL	3.6734 mL	7.3468 mL	18.3670 mL
	15 mM	0.4898 mL	2.4489 mL	4.8979 mL	12.2446 mL
	20 mM	0.3673 mL	1.8367 mL	3.6734 mL	9.1835 mL
	25 mM	0.2939 mL	1.4694 mL	2.9387 mL	7.3468 mL
	30 mM	0.2449 mL	1.2245 mL	2.4489 mL	6.1223 mL
	40 mM	0.1837 mL	0.9183 mL	1.8367 mL	4.5917 mL
	50 mM	0.1469 mL	0.7347 mL	1.4694 mL	3.6734 mL
	60 mM	0.1224 mL	0.6122 mL	1.2245 mL	3.0612 mL
	80 mM	0.0918 mL	0.4592 mL	0.9183 mL	2.2959 mL
	100 mM	0.0735 mL	0.3673 mL	0.7347 mL	1.8367 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.

Keywords

Allopurinol

12 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) Allopurinol

Activité biologique

Chemical Information

Publications (12)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Allopurinol Related Classifications

HY-B0219 Related Classifications