1. Epigenetics Apoptosis
  2. MicroRNA Apoptosis
  3. Targapremir-210

Targapremir-210  (Synonyms: TGP-210)

Cat. No.: HY-15861 Purity: 98.00%
COA Handling Instructions

Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM). Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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

Targapremir-210 Chemical Structure

Targapremir-210 Chemical Structure

CAS No. : 1049722-30-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 340 In-stock
Solution
10 mM * 1 mL in DMSO USD 340 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 460 In-stock
25 mg USD 920 In-stock
50 mg USD 1650 In-stock
100 mg USD 2800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM)[1]. Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

IC50 & Target

IC50: 200 nM (miR-210, in MDA-MB-231 cells)[1].

In Vitro

Targapremir-210 decreases mature miR-210 levels in MDA-MB-231 cells cultured under hypoxic conditions, with an IC50 of ~200 nM[1].
Targapremir-210 (200 nM) induces MDA-MB-231 cells apoptosis is selective for the hypoxic environment. Targapremir-210 induces cells apoptosis under hypoxic conditions and does not induce apoptosis in MDA-MB-231 cells cultured in normoxia[1].

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

In Vivo

Targapremir-210 (100 μL of 200 nM; single i.p. injection) impedes MDA-MB-231 triple negative breast cancer (TNBC) cells proliferation in vivo. Targapremir-210 is able to reach the tumor and sustain for the entire 21-day period, and decreases tumor burden in a TNBC mouse model[1].

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

Animal Model: NOD/SCID mice were subcutaneously transplanted cell suspension into breast fat pads[1].
Dosage: 100 μL of 200 nM
Administration: Single i.p. injection 24 h post-transplantation
Result: Decreased tumor growth as assessed by luciferase signal intensity and mass of the resected tumor.
Molecular Weight

592.69

Formula

C32H36N10O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NCCCN=[N+]=[N-])CCCOC1=CC=CC(C2=NC3=CC=C(C4=NC5=CC=C(N6CCN(C)CC6)C=C5N4)C=C3N2)=C1

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 : 250 mg/mL (421.81 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 1.6872 mL 8.4361 mL 16.8722 mL
5 mM 0.3374 mL 1.6872 mL 3.3744 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.

  • 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: ≥ 2.08 mg/mL (3.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (3.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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)

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
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
DMSO 1 mM 1.6872 mL 8.4361 mL 16.8722 mL 42.1806 mL
5 mM 0.3374 mL 1.6872 mL 3.3744 mL 8.4361 mL
10 mM 0.1687 mL 0.8436 mL 1.6872 mL 4.2181 mL
15 mM 0.1125 mL 0.5624 mL 1.1248 mL 2.8120 mL
20 mM 0.0844 mL 0.4218 mL 0.8436 mL 2.1090 mL
25 mM 0.0675 mL 0.3374 mL 0.6749 mL 1.6872 mL
30 mM 0.0562 mL 0.2812 mL 0.5624 mL 1.4060 mL
40 mM 0.0422 mL 0.2109 mL 0.4218 mL 1.0545 mL
50 mM 0.0337 mL 0.1687 mL 0.3374 mL 0.8436 mL
60 mM 0.0281 mL 0.1406 mL 0.2812 mL 0.7030 mL
80 mM 0.0211 mL 0.1055 mL 0.2109 mL 0.5273 mL
100 mM 0.0169 mL 0.0844 mL 0.1687 mL 0.4218 mL
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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.

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Targapremir-210
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