Art. -Nr.: HY-106841

Draflazine

(Synonyms: R-75231; R88021)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

Draflazine (R-75231) is a ENT1 inhibitor. Draflazine (R-75231) completely reverses the hypersensitivity in the complete Freund’s adjuvant (CFA) model of mechanical hyperalgesia and the carrageenan inflammation model of thermal and mechanical hyperalgesia.

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Reinheit: 99.06%
CAS. Nr.: 120770-34-5
Formel: C₃₀H₃₃Cl₂F₂N₅O₂
Molecular Weight:604.52

Speicherung:

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

Draflazine Chemical Structure

CAS. Nr.: 120770-34-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

ENT1^[1]

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
U2OS	IC₅₀	5.3 nM Compound: 60849	Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay	[PMID: 31551431]
U2OS	IC₅₀	5.3 nM Compound: 60849	Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay (PubChem AID: 1745861) Inhibition of the equilibrative nucleoside transporter (ENT1, SLC29A1) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay (PubChem AID: 1745861)	[PMID: 31551431]

Chemical Information

CAS. Nr. 120770-34-5
Appearance Solid
Molecular Weight 604.52
Formel C₃₀H₃₃Cl₂F₂N₅O₂
Color White to off-white
SMILES

O=C(NC1=C(Cl)C=C(N)C=C1Cl)CN2C(C(N)=O)CN(CCCCC(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2
Synonyms

R-75231; R88021
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

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Journal Impact Factor

bioRxiv

2026 Jan 27.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (165.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

1.6542 mL

8.2710 mL

16.5420 mL

5 mM

0.3308 mL

1.6542 mL

3.3084 mL

10 mM

0.1654 mL

0.8271 mL

1.6542 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.14 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (4.14 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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Maes SS, et al. Antihyperalgesic activity of nucleoside transport inhibitors in models of inflammatory pain in guinea pigs. J Pain Res. 2012;5:391-400. [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
DMSO	1 mM	1.6542 mL	8.2710 mL	16.5420 mL	41.3551 mL
	5 mM	0.3308 mL	1.6542 mL	3.3084 mL	8.2710 mL
	10 mM	0.1654 mL	0.8271 mL	1.6542 mL	4.1355 mL
	15 mM	0.1103 mL	0.5514 mL	1.1028 mL	2.7570 mL
	20 mM	0.0827 mL	0.4136 mL	0.8271 mL	2.0678 mL
	25 mM	0.0662 mL	0.3308 mL	0.6617 mL	1.6542 mL
	30 mM	0.0551 mL	0.2757 mL	0.5514 mL	1.3785 mL
	40 mM	0.0414 mL	0.2068 mL	0.4136 mL	1.0339 mL
	50 mM	0.0331 mL	0.1654 mL	0.3308 mL	0.8271 mL
	60 mM	0.0276 mL	0.1379 mL	0.2757 mL	0.6893 mL
	80 mM	0.0207 mL	0.1034 mL	0.2068 mL	0.5169 mL
	100 mM	0.0165 mL	0.0827 mL	0.1654 mL	0.4136 mL

Keywords

Draflazine

1 Cited Publications

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Draflazine

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Publications Citing Use of MedChemExpress (MCE) Draflazine

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Draflazine

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Small Molecule Immuno-Oncology Compound Library

Drug Repurposing Compound Library

Neurotransmitter Receptor Compound Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Immunopotentiator Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Draflazine

Alle Adenosine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Draflazine Related Classifications

HY-106841 Related Classifications