| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PAI-1 (IC50 = 26.1 μM); KATP; ERK; JNK
Loureirin B targets multiple molecular targets. It inhibits plasminogen activator inhibitor-1 (PAI-1) with an IC50 of 26.10 μM. It also inhibits KATP channels and Kv1.3 channels. It inhibits phosphorylation of ERK and JNK. It modulates the TGF-β1/Smad2/3 pathway. |
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| ln Vitro |
Loureirin B enhances the relative mRNA level of Pdx-1 and MafA. Insulin secretion from Ins-1 cells is boosted by loureirin B (1, 0.1, and 0.01 µM). Cells are almost completely unaffected by loureirin B (0.01 µM). The expression of MafA, Pdx-1, and ATP are all enhanced by Loureirin B. While increasing the [Ca2+]i level in Ins-1 cells, loureirin B inhibits the KATP current[1]. The TGF-β1-mediated upregulation of p-JNK as well as the expression of Col1 and FN are all inhibited by loureirin B. p-ERK is upregulated by TGF-β1, and loureirin B inhibits this process. The downregulation of p-ERK and p-JNK is another way that loureirin B prevents the contraction of TGF-β1 stimulated fibroblasts. The upregulation of p-p38 brought on by TGF-β1 is not suppressed by loureirin B, though [2]. Type I collagen, type III collagen, and -smooth muscle actin have dose-dependent downregulations by loureirin B at the mRNA and protein levels in HS fibroblasts. Although it has no effect on cell apoptosis, loureirin B also reduces fibroblast proliferative activity and redistributes the cell cycle[3].
Loureirin B inhibits PAI-1 with an IC50 of 26.10 μM. It inhibits KATP current but increases [Ca2+]i levels in Ins-1 cells. It inhibits the expression of Col1 and FN, as well as TGF-β1-mediated upregulation of p-JNK. It downregulates fibrosis-related molecules by regulating MMPs and TIMPs. |
| ln Vivo |
In a rabbit ear scar model, loureirin B significantly improves collagen fiber arrangement and deposition, lowers ColI, ColIII, and -SMA protein levels, and suppresses myofibroblast differentiation and scar proliferative activity. The TGF-β1-induced upregulation of ColI, ColIII, and -SMA levels, myofibroblast differentiation, and activation of Smad2 and Smad3 in NS fibroblasts are all successfully inhibited by loureirin B[3].
Loureirin B has anti-diabetic activity. It improves the expression of MafA and Pdx-1 and ATP levels. It inhibits scar fibroblast proliferation and suppresses TGF-β1-induced fibrosis. It modulates sodium currents in trigeminal ganglion neurons. |
| Enzyme Assay |
Non-cell-based enzyme assays for Loureirin B use purified PAI-1 protein. The compound is incubated with PAI-1 and its target protease (e.g., tPA or uPA). Inhibition of PAI-1 activity is measured by assessing the remaining protease activity using chromogenic or fluorogenic substrates. IC50 values for PAI-1 inhibition are determined. KATP channel binding studies may be performed using membrane preparations.
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| Cell Assay |
On 96-well plates, Ins-1 cells are seeded and cultured for 48 hours until they are 80–90% confluent. The cells are then starved for 12 hours in a 2% FBS/DMEM solution. While the positive control group receives fresh medium containing glimepiride, the control group is cultured in medium devoid of loureirin B. Cell Counting Kit-8 (CCK-8) is used to determine the cell viability following treatments with loureirin B and glimepiride for 4 and 8 hours, respectively.
Cellular assays for Loureirin B utilize various cell types including Ins-1 cells (pancreatic beta cells), fibroblasts, and keratinocytes. Cells are treated with the compound at various concentrations. Endpoints include measurement of intracellular calcium levels ([Ca2+]i), KATP current by patch-clamp, PAI-1 activity in cell lysates or supernatants, and expression of fibrosis-related genes (e.g., Col1, FN, TGF-β1) by qPCR or Western blotting. |
| Animal Protocol |
In brief, 10 adult male New Zealand white rabbits (weighing between 2.0 and 2.5 kg each) are acclimated and housed in a 12-hour light/dark cycle with free access to water and SPF base diet. A dermal punch biopsy (10×4 mm) is made on the ventral surface of each ear of the rabbit to outline a full-thickness wound after the animal has been given 1% pentobarbital (1.5 mg/kg b.w.) anesthesia. On each of the eight rabbits' ears, four punches are made. To ensure that the epidermis, dermis, and perichondrium are completely removed from each wound, a dissecting microscope is employed. DMSO solution (0.125% in PBS, 0.25 mL/kg b.w.) is subcutaneously injected into the left ear of each group of injured rabbits 48 hours after surgery, and loureirin B solution (25 g/mL in PBS, 0.25 mL/kg b.w.) is subcutaneously injected into the right ear once every other day for a total of six times. Two rabbits are used in the pilot study, four are sacrificed at 14 days following the injury (n = 4), and the remaining four are sacrificed at 28 days following the injury (n = 4). The same ear contains four scar tissues, two of which are processed for Western blot and the other two for Masson staining.
In vivo animal models for Loureirin B include models of diabetes, fibrosis, and wound healing. The compound is administered orally or via other routes. Efficacy is assessed by measuring blood glucose levels, insulin secretion, fibrosis markers in tissues, and wound healing parameters. Detailed protocols are not extensively reported. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Loureirin B include CAS number 119425-90-0. The compound is a flavonoid natural product. It has poor water solubility. Detailed PK parameters such as half-life and bioavailability are not extensively reported. The compound is a bioactive drug used in research.
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| Toxicity/Toxicokinetics |
Loureirin B has anti-diabetic, anti-fibrotic, and anti-inflammatory activities. It is a natural product with multiple targets. Detailed toxicity data are not extensively reported. As a natural product, it may have a more favorable safety profile than synthetic compounds. It has poor water solubility.
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| References |
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| Additional Infomation |
Loureirin B belongs to the dihydrochalcone class of compounds. It has been reported that Loureirin B exists in Garcinia dulcis, and relevant data are available for reference.
Loureirin B is a flavonoid isolated from Dracaena cochinchinensis. It has CAS number 119425-90-0. It is a PAI-1 inhibitor (IC50 = 26.10 μM) and also inhibits KATP channels and ERK/JNK phosphorylation. It has anti-diabetic activity and anti-fibrotic effects. It is a research compound for diabetes and fibrosis studies. |
| Molecular Formula |
C18H20O5
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|---|---|
| Molecular Weight |
316.35
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| Exact Mass |
316.131
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| Elemental Analysis |
C, 68.34; H, 6.37; O, 25.29
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| CAS # |
119425-90-0
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| Related CAS # |
119425-90-0
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| PubChem CID |
189670
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
509.9±50.0 °C at 760 mmHg
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| Flash Point |
184.0±23.6 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.564
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| LogP |
2.98
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
350
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C([H])([H])[H])C1C([H])=C(C([H])=C(C=1C([H])([H])C([H])([H])C(C1C([H])=C([H])C(=C([H])C=1[H])O[H])=O)OC([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
ZPFRAPVRYLGYEC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20O5/c1-21-14-10-17(22-2)15(18(11-14)23-3)8-9-16(20)12-4-6-13(19)7-5-12/h4-7,10-11,19H,8-9H2,1-3H3
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| Chemical Name |
1-(4-hydroxyphenyl)-3-(2,4,6-trimethoxyphenyl)propan-1-one
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| Synonyms |
L B; LR-B; Loureirin B
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 150 mg/mL (~474.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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