Draflazine (Synonyms: R-75231; R88021)

Cat. No.: HY-106841 Purity: 99.06%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Draflazine Chemical Structure

CAS No. : 120770-34-5

Size	Price	Stock
5 mg	USD 410	Ask For Quote & Lead Time
10 mg	USD 670	Ask For Quote & Lead Time
25 mg	USD 1340	Ask For Quote & Lead Time
50 mg	USD 2150	Ask For Quote & Lead Time
100 mg	USD 3500	Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

Other Forms of Draflazine:

(S)-Draflazine Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

ENT1^[1]

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]

Molecular Weight

604.52

Formula

C₃₀H₃₃Cl₂F₂N₅O₂

CAS No.

120770-34-5

Appearance

Solid

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

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

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

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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: ≥ 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.
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 (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.
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: ≥ 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

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.

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: 99.06%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (250 KB) HNMR (147 KB) RP-HPLC (172 KB) LCMS (392 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Draflazine Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Draflazine120770-34-5R-75231 R88021R75231R 75231R88021R 88021R-88021OthersInhibitorinhibitorinhibit

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