CNT2 inhibitor-1

Name: CNT2 inhibitor-1
Brand: MedChemExpress
SKU: HY-112843
Rating: 4.5 (1 reviews)

Cat. No.: HY-112843 Purity: 98.77%: FAQs
Data Sheet SDS COA Handling Instructions

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CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC₅₀ of 640 nM for hCNT2.

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

CNT2 inhibitor-1 Chemical Structure

CAS No. : 880155-70-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 434	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 434	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 395	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 592	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1066	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1600	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2400	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Description

CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC₅₀ of 640 nM for hCNT2.

IC₅₀ & Target

IC50: 640 nM (hCNT2)^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	0.64 μM Compound: 1	Inhibition of human CNT2 expressed in African green monkey COS7 cells assessed as reduction of [14C]-inosine uptake by liquid scintillation counting analysis Inhibition of human CNT2 expressed in African green monkey COS7 cells assessed as reduction of [14C]-inosine uptake by liquid scintillation counting analysis	[PMID: 27007871]
COS-7	IC₅₀	0.64 μM Compound: 48	Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake in presence of Na+ by liquid scintillation counting method Inhibition of human CNT2 expressed in COS7 cells assessed as reduction in sodium-dependent [14C]-inosine uptake in presence of Na+ by liquid scintillation counting method	[PMID: 25815140]

In Vitro

CNT2 inhibitor-1 (compound 48) exhibits 81-fold more potent inhibitory activity than the parent compound 12. In addition, CNT2 inhibitor-1 exhibits inhibitory activity 1500-fold more potent than that of 2’-deoxy-5-fluorouridine, phlorizin, and 7,8,3’-trihydroxyflavone, which are well-known hCNT2 inhibitors^[1]. CNT2 inhibitor-1 (compound 1) is a potent inhibitor with poor solubility^[2].

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

Molecular Weight

448.47

Formula

C₂₃H₂₄N₆O₄

CAS No.

880155-70-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

OC[C@@H]1[C@H]([C@H]([C@H](N2C(NCC3=CC=C(C4=CC=CC=C4)C=C3)=NC5=C2N=CN=C5N)O1)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 : 75 mg/mL (167.24 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	2.2298 mL	11.1490 mL	22.2980 mL
5 mM	0.4460 mL	2.2298 mL	4.4596 mL
10 mM	0.2230 mL	1.1149 mL	2.2298 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.

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: ≥ 2.5 mg/mL (5.57 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 (5.57 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.

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: 98.77%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (252 KB) HNMR (190 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[1]. Tatani K, et al. Identification of 8-aminoadenosine derivatives as a new class of human concentrative nucleoside transporter 2 inhibitors. ACS Med Chem Lett. 2015 Jan 28;6(3):244-8. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2298 mL	11.1490 mL	22.2980 mL	55.7451 mL
	5 mM	0.4460 mL	2.2298 mL	4.4596 mL	11.1490 mL
	10 mM	0.2230 mL	1.1149 mL	2.2298 mL	5.5745 mL
	15 mM	0.1487 mL	0.7433 mL	1.4865 mL	3.7163 mL
	20 mM	0.1115 mL	0.5575 mL	1.1149 mL	2.7873 mL
	25 mM	0.0892 mL	0.4460 mL	0.8919 mL	2.2298 mL
	30 mM	0.0743 mL	0.3716 mL	0.7433 mL	1.8582 mL
	40 mM	0.0557 mL	0.2787 mL	0.5575 mL	1.3936 mL
	50 mM	0.0446 mL	0.2230 mL	0.4460 mL	1.1149 mL
	60 mM	0.0372 mL	0.1858 mL	0.3716 mL	0.9291 mL
	80 mM	0.0279 mL	0.1394 mL	0.2787 mL	0.6968 mL
	100 mM	0.0223 mL	0.1115 mL	0.2230 mL	0.5575 mL

CNT2 inhibitor-1 Related Classifications

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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:

CNT2 inhibitor-1880155-70-4OthersInhibitorinhibitorinhibit

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CNT2 inhibitor-1

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Complete Stock Solution Preparation Table

CNT2 inhibitor-1 Related Classifications

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