LIT-927

Product Name: LIT-927
CAS No.: 2172879-52-4
Chemical Name: LIT-927
Synonyms: LIT-927;CS-2869;LIT-927 ，S8813;LIT927, 10 mM in DMSO;4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)-2(1H)-pyridone;4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)pyrimidin-2(1H)-one;2(1H)-Pyrimidinone, 4-(4-chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)-
CBNumber: CB94668137
Molecular Formula: C17H13ClN2O3
Formula Weight: 328.75
MOL File: 2172879-52-4.mol

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LIT-927 Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2893
Product name: LIT-927
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $94.2
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML2893
Product name: LIT-927
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $306
Updated: 2024/03/01

Cayman Chemical

Product number: 28436
Product name: LIT-927
Packaging: 5mg
Price: $93
Updated: 2024/03/01

Cayman Chemical

Product number: 28436
Product name: LIT-927
Packaging: 50mg
Price: $547
Updated: 2024/03/01

Cayman Chemical

Product number: 28436
Product name: LIT-927
Packaging: 10mg
Price: $146
Updated: 2024/03/01

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LIT-927 Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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LIT-927 Suppliers

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2172879-52-4, LIT-927Related Search:

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

2172879-52-4

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