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LIT-927 Sale

(Synonyms: LIT-927游离) 目录号 : GC19486

A neutraligand of CXCL12

LIT-927  Chemical Structure

Cas No.:2172879-52-4

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5mg
¥556.00
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25mg
¥1,663.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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] .

LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12 binding to CXCR4. Compounds 50, 57 (LIT-927), 65, and 67 are the most potent and soluble cyclic neutraligands identified in vitro and are representative of four novel chemotypes: pyrazoline, pyrimidinone, benzofuranone, and chromanone. LIT-927 is bound to a wide and accessible pocket, which is incompatible with the observed nanomolar binding affinities of our neutraligands[1].

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].

Reference:

[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.

Chemical Properties

Cas No. 2172879-52-4 SDF
别名 LIT-927游离
Canonical SMILES ClC1=CC=C(C(C=C(C2=CC=C(O)C(OC)=C2)N3)=NC3=O)C=C1
分子式 C₁₇H₁₃ClN₂O₃ 分子量 328.75
溶解度 DMF: 1mg/mL 储存条件 Store at -20°C
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1 mM 3.0418 mL 15.2091 mL 30.4183 mL
5 mM 0.6084 mL 3.0418 mL 6.0837 mL
10 mM 0.3042 mL 1.5209 mL 3.0418 mL
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