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

Loureirin B 

Cat. No.: HY-N1504 Purity: 99.99%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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

IC50: 26.10 μM (PAI-1)[4]

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].

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].

Molecular Weight

316.35

Formula

C₁₈H₂₀O₅

CAS No.

119425-90-0

SMILES

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

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 : ≥ 150 mg/mL (474.16 mM)

*"≥" 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
10 mM 0.3161 mL 1.5805 mL 3.1611 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Keywords:

Loureirin BPAI-1Potassium ChannelERKJNKPlasminogen activator inhibitor-1KcsAExtracellular signal regulated kinasesc-Jun N-terminal kinaseInhibitorinhibitorinhibit

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Loureirin B
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