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  4. LDN-27219

LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease.

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

LDN-27219 Chemical Structure

LDN-27219 Chemical Structure

CAS No. : 312946-37-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

LDN-27219 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE LDN-27219

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease[1][2].

IC50 & Target

IC50: 0.6 μM (hTGase)[1]
In Vitro

LDN-27219 (30 μM; 12 min) promotes the closed conformation of TGase 2 to activates calcium-activated potassium channels in smooth muscle cells[2].
LDN-27219 (30 μM; 20-25 min) increases the response to acetylcholine in phenylephrine-contracted human subcutaneous arteries[2].

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

LDN-27219 Related Antibodies
In Vivo

LDN-27219 (0.1-2 mg/kg; i.v. once) affects vivo arterial pressure and shows larger effects on older rats[2].

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

Animal Model: 12 to 14-week-old male Wistar rats[2]
Dosage: 0.1, 1 and 2 mg/kg
Administration: Intravenous injection; 0.1, 1 and 2 mg/kg once
Result: Dose-dependently decreased mean arterial pressure of mice.
Animal Model: 12 to 14- and 35 to 40-week-old male Wistar rats
Dosage: 0.1, 1 and 2 mg/kg
Administration: Intravenous injection; 0.1, 1 and 2 mg/kg once
Result: Decreased mean arterial pressure in old group more significant than young group.
Molecular Weight

408.50

Formula

C20H16N4O2S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(C2=CC=CC=C2)C(SCC(NN)=O)=NC3=C1C(C4=CC=CC=C4)=CS3
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 : 100 mg/mL (244.80 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 2.4480 mL 12.2399 mL 24.4798 mL
5 mM 0.4896 mL 2.4480 mL 4.8960 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 2.5 mg/mL (6.12 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: ≥ 2.08 mg/mL (5.09 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

Purity: 99.64%

SDS (393 KB)

COA (254 KB) HNMR (263 KB) LCMS (104 KB)

Handling Instructions (2659 KB)
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 2.4480 mL 12.2399 mL 24.4798 mL 61.1995 mL
5 mM 0.4896 mL 2.4480 mL 4.8960 mL 12.2399 mL
10 mM 0.2448 mL 1.2240 mL 2.4480 mL 6.1200 mL
15 mM 0.1632 mL 0.8160 mL 1.6320 mL 4.0800 mL
20 mM 0.1224 mL 0.6120 mL 1.2240 mL 3.0600 mL
25 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4480 mL
30 mM 0.0816 mL 0.4080 mL 0.8160 mL 2.0400 mL
40 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5300 mL
50 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2240 mL
60 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0200 mL
80 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7650 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 mL
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LDN-27219 Related Classifications

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:

LDN-27219312946-37-5LDN27219LDN 27219Othersreversibleslow-bindingvasodilationsmooth muscle cellarterial pressureratInhibitorinhibitorinhibit

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