1. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Stem Cell/Wnt MAPK/ERK Pathway
  2. PAI-1 Potassium Channel ERK JNK
  3. Loureirin B

Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.

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

Loureirin B Chemical Structure

Loureirin B Chemical Structure

CAS No. : 119425-90-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 198 In-stock
Solution
10 mM * 1 mL in DMSO USD 198 In-stock
Solid
1 mg USD 85 In-stock
5 mg USD 180 In-stock
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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.

IC50 & Target[1][2][4]

PAI-1

26.1 μM (IC50)

KATP

 

ERK

 

JNK

 

In Vitro

Loureirin B enhances the relative mRNA level of Pdx-1 and MafA. Loureirin B (1, 0.1, and 0.01 µM) increases insulin secretion in Ins-1 cells. Loureirin B (0.01 µM) almost causes no toxicity on cells. Loureirin B improves the level of expressions of MafA and Pdx-1 and ATP level. Loureirin B inhibits the KATP current but increases the [Ca2+]i level in Ins-1 cells[1]. Loureirin B inhibits the expression of Col1 and FN, as well as the TGF-β1-mediated up regulation of p-JNK. Loureirin B also inhibits the up regulation of p-ERK that is induced by TGF-β1. Moreover, Loureirin B inhibits the contraction of TGF-β1-stimulated fibroblasts through the down regulation of p-ERK and p-JNK. However, Loureirin B does not suppress the up regulation of p-p38 that is induced by TGF-β1[2]. Loureirin B downregulates both mRNA and protein levels of type I collagen, type III collagen and α-smooth muscle actin in a dose dependent manner in HS fibroblasts. Loureirin B also suppresses fibroblast proliferative activity and redistributes cell cycle, but does not affect cell apoptosis[3].

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

In Vivo

Loureirin B significantly improves the arrangement and deposition of collagen fibres, decreases protein levels of ColI, ColIII and α-SMA and suppresses myofibroblast differentiation and scar proliferative activity, in a rabbit ear scar model. Loureirin B effectively inhibits TGF-β1-induced upregulation of ColI, ColIII and α-SMA levels, myofibroblast differentiation and the activation of Smad2 and Smad3, in NS fibroblasts[3].

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

Molecular Weight

316.35

Formula

C18H20O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(O)C=C1)CCC2=C(OC)C=C(OC)C=C2OC

Structure Classification
Initial Source
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 : ≥ 150 mg/mL (474.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1611 mL 15.8053 mL 31.6106 mL
5 mM 0.6322 mL 3.1611 mL 6.3221 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: ≥ 2.5 mg/mL (7.90 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 (7.90 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:

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mg/kg

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(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: 99.16%

References
Cell Assay
[1]

Ins-1 cells are seeded onto 96-well plates and cultured for 48 h to approximately 80-90% confluence. Then, the cells are starved in a 2% FBS/DMEM for 12 h. Control group is cultured in medium without loureirin B, while the positive control group is received fresh medium with glimepiride. After the treatment of loureirin B and glimepiride for 4 and 8 h, the cell viability is measured by Cell Counting Kit-8 (CCK-8).

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

Animal Administration
[3]

For short, 10 adult New Zealand white male rabbits (2.0-2.5 kg b.w./each) are acclimated and housed under the standard 12-h light: 12-h dark cycle with free access of water and SPF basal diet. Rabbit is first anaesthetized with 1% pentobarbital (1.5 mg/kg b.w.), and then, a dermal punch biopsy (10×4 mm) is created down to bare cartilage on the ventral surface of each ear to outline a full-thickness wound. Four punch wounds are made on each ear of the eight rabbits. A dissecting microscope is used to ensure the complete removal of epidermis, dermis and perichondrium in each wound. Forty-eight hours after surgery, wounded rabbits are randomLy divided into two groups with each being subcutaneously injected with DMSO solution (0.125% in PBS, 0.25 mL/kg b.w.) on the left ear or loureirin B solution (25 μg/mL in PBS, 0.25 mL/kg b.w.) on the right ear once every other day for total six times. Two rabbits are used for pilot experiment, four rabbits are sacrificed 14 days after injury (n = 4), and the rest four are sacrificed 28 days after injury (n=4). Two of the four scar tissues on the same ear are processed for Western blot, and the other two are used for Masson staining.

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

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 3.1611 mL 15.8053 mL 31.6106 mL 79.0264 mL
5 mM 0.6322 mL 3.1611 mL 6.3221 mL 15.8053 mL
10 mM 0.3161 mL 1.5805 mL 3.1611 mL 7.9026 mL
15 mM 0.2107 mL 1.0537 mL 2.1074 mL 5.2684 mL
20 mM 0.1581 mL 0.7903 mL 1.5805 mL 3.9513 mL
25 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1611 mL
30 mM 0.1054 mL 0.5268 mL 1.0537 mL 2.6342 mL
40 mM 0.0790 mL 0.3951 mL 0.7903 mL 1.9757 mL
50 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5805 mL
60 mM 0.0527 mL 0.2634 mL 0.5268 mL 1.3171 mL
80 mM 0.0395 mL 0.1976 mL 0.3951 mL 0.9878 mL
100 mM 0.0316 mL 0.1581 mL 0.3161 mL 0.7903 mL
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