| Company Name: |
Sigma-Aldrich |
| Tel: |
021-61415566 800-8193336 |
| Email: |
orderCN@merckgroup.com |
- LIT-927
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2026-07-22
- CAS:2172879-52-4
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 1000kg
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| | LIT-927 Basic information |
| Product Name: | LIT-927 | | Synonyms: | CS-2869;LIT-927;2(1H)-Pyrimidinone, 4-(4-chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)-;4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)pyrimidin-2(1H)-one;LIT927, 10 mM in DMSO;LIT-927 ，S8813;4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)-2(1H)-pyridone | | CAS: | 2172879-52-4 | | MF: | C17H13ClN2O3 | | MW: | 328.75 | | EINECS: | | | Product Categories: | API | | Mol File: | 2172879-52-4.mol |  |
| | LIT-927 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO:66.0(Max Conc. mg/mL);200.76(Max Conc. mM) | | form | A solid | | color | Light yellow to yellow |
| | LIT-927 Usage And Synthesis |
| Uses | LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12 binding to its specific receptor CXCR4[1] . | | Biochem/physiol Actions | LIT-927 is an orally active CXCL12 (SDF1) neutraligand (Kd = 267) that selectively neutralizes CXCL12, but not CCL17, CCL22, CCL5, or CCL2 activity in cultures (10 μM LIT-927 against 5 nM chemokine-induced calcium mobilization). LIT-927 reduces eosinophil recruitment in a murine allergic airway hypereosinophilia model in vivo (330 nmol/kg intranasal, 350 nmol/kg ip. or 1400 μmol/kg po.), offering greatly improved oral activity and solubility than Chalcone-4, and exhibiting little side-effects when compared with dexamethasone or CXCR4 antagonist AMD3100. | | in vivo | LIT-927 (compound 57) reduces eosinophil recruitment in a murine model of allergic airway hypereosinophilia, LIT-927 is the only one to display inhibitory activity following oral administration. Combined with a high binding selectivity for CXCL12 over other chemokines, LIT-927 represents a powerful pharmacological tool to investigate CXCL12 physiology in vivo and to explore the activity of chemokine neutralization in inflammatory and related diseases[1]. | | IC 50 | CXCL12/CXCR4: 267 nM (Ki) | | References | [1] Regenass P, et al. Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia. J Med Chem. 2018 Sep 13;61(17):7671-7686. DOI:10.1021/acs.jmedchem.8b00657 |
| | LIT-927 Preparation Products And Raw materials |
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