DLPC (Synonyms: 1,2Dilauroylsnglycero3Phosphocholine, 1,2-DLPC) |
Catalog No.GC14047
One-Click Copy Product Info
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DLPC (DLPC) is an LRH-1 agonist ligand.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 18194-25-7
Sample solution is provided at 25 µL, 10mM.
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DLPC is a medium-chain phosphatidylcholine and an agonist ligand of liver receptor homolog-1 (LRH-1)[1]. DLPC occupies the LRH-1 ligand-binding pocket and activates LRH-1-dependent transcriptional programs governing bile-acid synthesis, glucose and lipid metabolism, endoplasmic-reticulum stress resolution, macrophage polarization, and cellular differentiation[1,2,3,6]. DLPC is used in research on nuclear-receptor signaling, metabolic homeostasis, hepatic stress, inflammation, diabetes-associated kidney injury, and nervous-system tumor biology.
In vitro, DLPC (100μM; 24h) activated LRH-1 and increased cytochrome P450 family 8 subfamily B member 1 (CYP8B1) expression in C3A/HepG2 hepatoma cells[1]. DLPC (50μM; 4 or 24h) increased interleukin 10, transforming growth factor beta 1, interleukin 1 receptor antagonist, mannose receptor, Dectin-1, and CD36 expression in mouse peritoneal macrophages and promoted the LRH-1/cytochrome P450/15-hydroxyeicosatetraenoic acid/peroxisome proliferator-activated receptor gamma axis associated with alternative macrophage polarization[3]. DLPC (100μM; 24h) increased perilipin 5 (PLIN5) messenger ribonucleic acid and protein in HepG2 cells without increasing LRH-1 protein and enhanced an LRH-1-regulated program linked to hepatic triglyceride metabolism[4].
In vivo, DLPC (100mg/kg/day; oral gavage once daily for 3 weeks) reduced serum glucose and hepatic triglycerides, improved glucose tolerance and insulin sensitivity, and decreased hepatic steatosis in db/db mice[1]. DLPC (100mg/kg; oral gavage every 12h for four doses, twice before and twice after a single 1mg/kg tunicamycin intraperitoneal injection) increased polo-like kinase 3 and activating transcription factor 2 signaling, reduced hepatic lipid accumulation and apoptosis, and accelerated endoplasmic-reticulum stress resolution in mice[2]. DLPC (100mg/kg; oral gavage once daily for 13 days) reduced U87-MG xenograft growth, Ki67-positive proliferating cells, phosphorylated histone H3-positive mitotic cells, Nestin, and Vimentin in non-obese diabetic/severe combined immunodeficiency mice without increasing cleaved caspase 3[5]. DLPC (100mg/kg; oral gavage once daily for 3 weeks) increased glomerular LRH-1 and glutaminase 2 (GLS2), enhanced glutamine-to-glutamate conversion, reduced urinary albumin-to-creatinine ratio, podocyte foot-process fusion, glomerular lesions, and apoptosis, and restored podocyte number in db/db mice[6].
References:[1] Lee JM, Lee YK, Mamrosh JL, Busby SA, Griffin PR, Pathak MC, et al. A nuclear-receptor-dependent phosphatidylcholine pathway with antidiabetic effects. Nature. 2011;474(7352):506-510. doi:10.1038/nature10111.
[2] Mamrosh JL, Lee JM, Wagner M, Stambrook PJ, Whitby RJ, Sifers RN, et al. Nuclear receptor LRH-1/NR5A2 is required and targetable for liver endoplasmic reticulum stress resolution. eLife. 2014;3:e01694. doi:10.7554/eLife.01694.
[3] Lefevre L, Authier H, Stein S, Majorel C, Couderc B, Dardenne C, et al. LRH-1 mediates anti-inflammatory and antifungal phenotype of IL-13-activated macrophages through the PPARgamma ligand synthesis. Nat Commun. 2015;6:6801. doi:10.1038/ncomms7801.
[4] Pantha R, Lee JH, Bae JH, Koh EH, Shin M, Song DK, et al. Perilipin 5 is a novel target of nuclear receptor LRH-1 to regulate hepatic triglycerides metabolism. BMB Rep. 2021;54(9):476-481. doi:10.5483/BMBRep.2021.54.9.051.
[5] Gkikas D, Stellas D, Polissidis A, Manolakou T, Kokotou MG, Kokotos G, et al. Nuclear receptor NR5A2 negatively regulates cell proliferation and tumor growth in nervous system malignancies. Proc Natl Acad Sci U S A. 2021;118(39):e2015243118. doi:10.1073/pnas.2015243118.
[6] Hu J, Zhang Z, Hu H, Yang K, Zhu Z, Yang Q, et al. LRH-1 activation alleviates diabetes-induced podocyte injury by promoting GLS2-mediated glutaminolysis. Cell Prolif. 2023;56(11):e13479. doi:10.1111/cpr.13479.
| Cell experiment [1]: | |
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Cell lines |
Primary peritoneal macrophages from C57BL/6 mice |
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Preparation Method |
Dissolve DLPC in ethanol to prepare a stock solution and dilute it to 100μM with cell culture medium containing 10% charcoal-treated fetal bovine serum. Treat C3A/HepG2 cells with DLPC for 24h and use an equal volume of ethanol as the vehicle control. |
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Reaction Conditions |
50μM; 4 or 24h |
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Applications |
DLPC increased interleukin 10, transforming growth factor beta 1, interleukin 1 receptor antagonist, mannose receptor, Dectin-1, and CD36 expression and promoted LRH-1-dependent alternative macrophage polarization. |
| Animal experiment [2]: | |
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Animal models |
U87-MG glioblastoma xenografts in non-obese diabetic/severe combined immunodeficiency mice |
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Preparation Method |
Prepare the DLPC dosing formulation using ethanol and a vehicle composed of polyethylene glycol 400 (PEG-400) and Tween-80 at a ratio of 4:1. Administer DLPC to 12-week-old male db/db mice by oral gavage at 100mg/kg/day once daily for 3 weeks; administer an equal volume of vehicle to the control group. |
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Dosage form |
100mg/kg; 13 days; i.g. |
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Applications |
DLPC reduced xenograft volume and Ki67, phosphorylated histone H3, Nestin, and Vimentin levels without increasing cleaved caspase 3. |
| References: [1] Lefevre L, Authier H, Stein S, Majorel C, Couderc B, Dardenne C, et al. LRH-1 mediates anti-inflammatory and antifungal phenotype of IL-13-activated macrophages through the PPARgamma ligand synthesis. Nat Commun. 2015;6:6801. doi:10.1038/ncomms7801. [2] Gkikas D, Stellas D, Polissidis A, Manolakou T, Kokotou MG, Kokotos G, et al. Nuclear receptor NR5A2 negatively regulates cell proliferation and tumor growth in nervous system malignancies. Proc Natl Acad Sci U S A. 2021;118(39):e2015243118. doi:10.1073/pnas.2015243118. | |
| Cas No. | 18194-25-7 | SDF | |
| Synonyms | 1,2Dilauroylsnglycero3Phosphocholine, 1,2-DLPC | ||
| Chemical Name | (R)-2,3-bis(dodecanoyloxy)propyl (2-(trimethylammonio)ethyl) phosphate | ||
| Canonical SMILES | O=C(CCCCCCCCCCC)O[C@@H](CO[P@](OCC[N+](C)(C)C)([O-])=O)COC(CCCCCCCCCCC)=O | ||
| Formula | C32H64NO8P | M.Wt | 621.83 |
| Solubility | 100 mg/mL in Ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6082 mL | 8.0408 mL | 16.0816 mL |
| 5 mM | 321.6 μL | 1.6082 mL | 3.2163 mL |
| 10 mM | 160.8 μL | 804.1 μL | 1.6082 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)