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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
13 Results for "
ATX/LPA
" in MedChemExpress (MCE) Product Catalog:
Products (13)
13 Results for "ATX/LPA" in MCE Product Catalog:
2
2 Cited Publications
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BI-2545, a chemical probe, is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively .
Synonyms: BLD-0409; PAT-409
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Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc .
Synonyms: IOA-289
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CRT0273750 is an autotaxin (ATX) inhibitor and modulates LPA levels in plasm (IC50 = 0.014 μM). CRT0273750 can be used in ATX/LPA-dependent models of cancer .
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HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM .
Cat. No.: HY-148291
CAS No.: 944265-88-7
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BrP-LPA sodium is a pan-opposite agent for lysophosphatidic acid (LPA). It has antagonistic activity against LPA1 (IC50 = 4520 nM), LPA2 (IC50 = 468 nM), LPA3, and LPA4. BrP-LPA sodium also has partial agonistic activity for LPA5, with its EC50 being 1282 nM. BrP-LPA sodium has ATX inhibitory activity. BrP-LPA sodium effectively inhibits the migration and invasion of breast cancer cells. BrP-LPA sodium achieves tumor regression and anti-angiogenesis in mice breast cancer xenograft model. BrP-LPA sodium can be used for the study of breast cancer .
Cat. No.: HY-173509
CAS No.: 2023027-81-6
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Infection Cardiovascular Disease Neurological Disease Cancer
ATX inhibitor 27 (Compound 31) is an ATX inhibitor. The IC50 values of ATX inhibitor 27 against human autotaxin (hATX) and lysophosphatidylcholine (LPC) are 13 nM and 23 nM, respectively. ATX inhibitor 27 reduces LPA levels in vivo by inhibiting ATX enzyme. ATX inhibitor 27 can be used in the study of ATX-LPA-related diseases such as inflammation, neurodegenerative diseases and cancer .
Cat. No.: HY-174267S
CAS No.: 3076224-81-9
Cat. No.: HY-126230
CAS No.: 1781233-84-8
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PAT-494 is an ATX inhibitor with significant activity in biochemical and plasma assays. PAT-494 can reduce LPA levels in rat plasma through oral administration. The structure-activity relationship study of PAT-494 shows that its binding mode with ATX is novel and it can effectively occupy the hydrophobic pockets and channels of ATX .
Cat. No.: HY-119601
CAS No.: 313685-55-1
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GRI918013 (compound 1) is a selective and competitive autotaxin (ATX/NPP2) inhibitor with anti-invasive and anti-metastatic activity. GRI918013 competitively binds to ATX, blocking lipid substrates such as lysophosphatidylcholine (LPC) from entering the ATX active site, thereby inhibiting ATX-mediated hydrolysis of LPC to lysophosphatidic acid (LPA), and consequently inhibiting ATX-LPA axis-related tumor cell invasion and metastasis. GRI918013 inhibits ATX-mediated hydrolysis of the LPL substrate FS-3 (IC50=31.42 nM, Ki=12.98 nM). GRI918013 can be used in research on cancer invasion and metastasis, such as melanoma, and can also serve as a tool compound for ATX-LPA axis-related diseases such as fibrotic diseases, neuropathic pain, and cholestatic pruritus .
Cat. No.: HY-126233A
CAS No.: 2650082-35-0
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PAT-347 sodium is an Autotaxin (ATX) inhibitor. ATX is a secretory enzyme that hydrolyzes lysophosphatidylcholine (LPC) and regulates lysophosphatidic acid (LPA) production in the blood .
Cat. No.: HY-W725737
CAS No.: 944313-05-7
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BrP-LPA is a LPA antagonist/ATX inhibitor. BrP-LPA shows pan-antagonist activity towards LPA1-4 GPCRs. BrP-LPA decreases blood vessel density. BrP-LPA dose-dependently inhibits Lysophosphatidic acid-induced head-dip counts. BrP-LPA exhibits anticancer activity against breast cancer, colon cancer, and lung cancer. BrP-LPA inhibits anxiety-like behavior .
Cat. No.: HY-167201
CAS No.: 633278-53-2
Synonyms: 2ccPA18:1
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2ccPA (2ccPA18:1) is a metabolically stabilized carba analog of cyclic phosphatidic acid (cPA). 2ccPA inhibits autotaxin (ATX)‑mediated lysophosphatidic acid (LPA) production, suppresses extracellular matrix biosynthesis and elevates intracellular cAMP in fibrogenic skin fibroblasts. 2ccPA protects oligodendrocytes from mitochondrial‑driven apoptosis, suppresses neuroinflammation and demyelination, modulates microglial polarization and promotes rapid‑platelet/fibrin‑dependent hemostasis and subsequent fibrinolytic transition following brain injury .
Cat. No.: HY-179580
CAS No.: 3047548-70-6
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EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
