Transfected Stable Cell Lines
Reliable | High-Performance | Wide Rage
Precision reporter, kinase, immune receptor, biosimilar, Cas9, and knockout stable cell lines for diverse applications.
| Cat.No. | Product Name | Price |
|---|---|---|
| CSC-RG0870 | Human LPAR1 Stable Cell Line-RH7777 | Inquiry |
| CSC-DC001599 | Panoply™ Human BUD31 Knockdown Stable Cell Line | Inquiry |
| CSC-DC003830 | Panoply™ Human CTTNBP2NL Knockdown Stable Cell Line | Inquiry |
| CSC-DC008806 | Panoply™ Human LPAR1 Knockdown Stable Cell Line | Inquiry |
| CSC-SC001599 | Panoply™ Human BUD31 Over-expressing Stable Cell Line | Inquiry |
| CSC-SC003830 | Panoply™ Human CTTNBP2NL Over-expressing Stable Cell Line | Inquiry |
| CSC-SC008806 | Panoply™ Human LPAR1 Over-expressing Stable Cell Line | Inquiry |
| CSC-RG1794 | Mouse LPAR1 Stable Cell Line - RH7777 | Inquiry |
| CSC-SC008806-1 | Human LPAR1 Stable Cell Line - Ba/F3 | Inquiry |
| Cat.No. | Product Name | Price |
|---|---|---|
| AD01973Z | Human BUD31 adenoviral particles | Inquiry |
| AD04392Z | Human CTTNBP2NL adenoviral particles | Inquiry |
| AD09279Z | Human LPAR1 adenoviral particles | Inquiry |
| LV00360Z | Human LPAR1 lentiviral particles | Inquiry |
| LV00361Z | Human LPAR1 lentiviral particles | Inquiry |
| LV06444L | human BUD31 (NM_003910) lentivirus particles | Inquiry |
| LV10029L | human CTTNBP2NL (NM_018704) lentivirus particles | Inquiry |
| Cat.No. | Product Name | Price |
|---|---|---|
| SHW002774 | shRNA set against Chicken LPAR1 (NM_001115082) | Inquiry |
| SHH023717 | shRNA set against Human EDG2(NM_057159.2) | Inquiry |
| SHH023737 | shRNA set against Human EDG2(NM_001401.3) | Inquiry |
| SHH023755 | shRNA set against Human EDG2(NM_057159.2) | Inquiry |
| SHH023771 | shRNA set against Rat Edg2(NM_053936.3) | Inquiry |
| SHH072461 | shRNA set against Rat G10(NM_053556.1) | Inquiry |
| SHH248486 | shRNA set against Human BUD31 (NM_003910.3) | Inquiry |
| SHH248490 | shRNA set against Mouse BUD31 (NM_001008705.1) | Inquiry |
| SHH248494 | shRNA set against Rat BUD31 (NM_053556.1) | Inquiry |
| SHH271721 | shRNA set against Human CTTNBP2NL (NM_018704.2) | Inquiry |
| SHH271725 | shRNA set against Mouse CTTNBP2NL (NM_030249.4) | Inquiry |
| SHH271729 | shRNA set against Rat CTTNBP2NL (NM_001107712.2) | Inquiry |
| SHH333403 | shRNA set against Mouse LPAR1 (NM_010336.2) | Inquiry |
| SHH333407 | shRNA set against Rat LPAR1 (NM_053936.3) | Inquiry |
| SHW007033 | shRNA set against Danio rerio BUD31 (NM_001003860) | Inquiry |
| SHW007131 | shRNA set against Danio rerio LPAR1 (NM_001004502) | Inquiry |
| Cat.No. | Product Name | Price |
|---|---|---|
| OE-PNDC000143 | Human LPAR1 Nanodisc | Inquiry |
| Cat.No. | Product Name | Price |
|---|---|---|
| MiUTR4H-TG02458 | CTTNBP2NL miRNA 3'UTR clone | Inquiry |
| CDCR314686 | Human LPAR1 ORF Clone(NM_057159.2) | Inquiry |
| CDCR248822 | Mouse Lpar1 ORF Clone(NM_010336.2) | Inquiry |
| CDFG007227 | Human LPAR1 cDNA Clone(NM_057159.2) | Inquiry |
| CDFH010583 | Human LPAR1 cDNA Clone(NM_001401.3) | Inquiry |
| CDCR058636 | Human LPAR1 ORF clone (NM_001401.3) | Inquiry |
| MiUTR3H-06002 | BUD31 miRNA 3'UTR clone | Inquiry |
| CDFR007356 | Rat Cttnbp2nl cDNA Clone(NM_001107712.2) | Inquiry |
| CDFR013646 | Rat Lpar1 cDNA Clone(NM_053936.3) | Inquiry |
| MiUTR1H-03106 | LPAR1 miRNA 3'UTR clone | Inquiry |
| MiUTR1M-02321 | BUD31 miRNA 3'UTR clone | Inquiry |
| MiUTR1R-01643 | LPAR1 miRNA 3'UTR clone | Inquiry |
| MiUTR1R-01997 | BUD31 miRNA 3'UTR clone | Inquiry |
| MiUTR3H-04838 | LPAR1 miRNA 3'UTR clone | Inquiry |
| CDFR013280 | Rat Bud31 cDNA Clone(NM_053556.1) | Inquiry |
| CDCS410258 | Human LPAR1 ORF Clone (BC036034) | Inquiry |
| CDCS414851 | Human CTTNBP2NL ORF Clone (BC016029) | Inquiry |
| CDCS410259 | Human LPAR1 ORF Clone (BC073167) | Inquiry |
| CDCR374431 | Rat Cttnbp2nl ORF Clone(NM_001107712.2) | Inquiry |
| CDCR380357 | Rat Bud31 ORF Clone(NM_053556.1) | Inquiry |
| CDCR271961 | Mouse Lpar1 ORF Clone(NM_172989.1) | Inquiry |
| CDCR263539 | Mouse Cttnbp2nl ORF Clone(NM_030249.4) | Inquiry |
| CDCR239710 | Mouse Cttnbp2nl ORF Clone(NM_001163333.1) | Inquiry |
| CDCR239709 | Mouse Cttnbp2nl ORF Clone(NM_001163332.1) | Inquiry |
| CDCR035836 | Mouse Bud31 ORF clone (NM_001008705.1) | Inquiry |
| CDCB196771 | Rabbit LOC103347662 ORF clone (XM_008254301.1) | Inquiry |
| CDCB189919 | Rabbit BUD31 ORF clone (XM_008248923.1) | Inquiry |
| CDCB187831 | Rabbit CTTNBP2NL ORF clone (XM_002715769.2) | Inquiry |
| CDCB184834 | Rabbit LPAR1 ORF clone (XM_008254984.1) | Inquiry |
| CDCB168606 | Danio rerio LPAR1 ORF Clone (NM_001004502) | Inquiry |
| CDCB168508 | Danio rerio BUD31 ORF Clone (NM_001003860) | Inquiry |
| CDCB164249 | Chicken LPAR1 ORF Clone (NM_001115082) | Inquiry |
| CDCR380519 | Rat Lpar1 ORF Clone(NM_053936.3) | Inquiry |
| CDCB156171 | Cynomolgus BUD31 ORF clone | Inquiry |
Lysophosphatidic acid receptor 1 (LPAR1), also known as Endothelial differentiation gene-2 receptor (Edg2), was first discovered in the developing brain in 1996. Research showed that LPAR1 is enriched in the ventricular zone (VZ) of the embryonic cerebral cortex. Subsequently, researchers identified five other receptors in the LPAR family, including LPAR2, LPAR3, LPAR4, LPAR5, and LPAR6, all of which are expressed in the central nervous system (CNS).
LPAR1 is a 41 kDa protein composed of 364 amino acids, with its gene located on human chromosome 9 (9q31.3). As a G protein-coupled receptor (GPCR) on the cell surface, LPAR1 has a seven-transmembrane structure, forming 3 extracellular loops and 3 intracellular loops. It has a putative nuclear translocation signal, an N-terminal acidic domain, and a cysteine-rich C-terminal domain containing a putative zinc finger structure. The polypeptide sequence of LPAR1 is highly conserved during evolution, suggesting that it may be an important regulator of general nuclear function.
LPAR1 is widely expressed in various tissues and organs of the human body, particularly with high mRNA levels in the brain, heart, colon, small intestine, and placenta, but relatively lower in other organs and tissues. In the central nervous system, LPAR1 is present on various cell types, such as astrocytes, oligodendrocytes, microglia, and neurons.
Figure 1. LPA signaling causes G proteins to play different roles in the CNS. (Xiao D, et al., 2021)
The ligand for LPAR1 is lysophosphatidic acid (LPA), a bioactive phospholipid with a 1-acyl-sn-glycerol-3-phosphate structure. LPA is an extracellular signaling molecule present in all eukaryotic tissues and plasma, produced during cell membrane synthesis, and mediates extracellular signal transduction through interaction with specific G protein-coupled receptors.
After binding to LPAR1, LPA couples with G proteins (Gi/0, Gαq, and G12/13), subsequently activating second messenger pathways, participating in the regulation of cell proliferation, migration, survival, apoptosis, and morphological changes. Specifically:
Notably, LPAR1 with the P308S, I310T, and Y311H mutations might not interact with helix 8, leading to structural defects and retention of LPAR1 in the endoplasmic reticulum. In addition, mutation of LPAR1 can alter its intracellular activities, such as Ca2+ mobilization, inhibition of cAMP formation, and cytoskeletal changes, which are mainly mediated by Gq, Gi/o, and G12/13, respectively.
The company with the fastest research in this field is BMS, with reported compounds including BMS-986020, BMS-986234, and BMS-986278. All three compounds are effective antagonists of LPA1 but have different chemical structures.
Phase II clinical trial (NCT01766817) results showed that, compared to placebo, IPF patients receiving BMS-986020 600 mg BID treatment had significantly slower decline in pulmonary fibrosis scores from baseline to 26 weeks. However, this Phase II trial was forced to terminate due to hepatobiliary toxicity in clinical subjects. In addition to hepatobiliary toxicity, BMS-986020 has an unstable structure and is easily metabolized, resulting in very large clinical doses.
After restructuring, researchers obtained BMS-986278. BMS-986278 exhibits ideal physicochemical properties and metabolic stability, effectively inhibits LPA-stimulated calcium flux in human lung fibroblasts, significantly inhibits bleomycin-induced pulmonary fibrosis, and has significantly reduced potential hepatotoxicity. According to the results reported by the European Respiratory Society in 2023, the FDA has granted BMS-986278 breakthrough therapy designation, and BMS-986278 is currently in Phase III trials in IPF patients.
Besides BMS, in 2023, Amgen spent $27.8 billion to acquire Horizon Therapeutics, thereby obtaining its LPAR1 target drug fipaxalparant (HZN-825), which is currently in Phase II clinical research (NCT05032066).
References