A neutraligand of CXCL12 (Ki = 267 nM in a FRET-based binding assay); selective for inhibiting calcium accumulation induced by CXCL12 over that induced by CCL17

LIT-927 – 25 mg

Brand:
Cayman
CAS:
2172879-52-4
Storage:
-20
UN-No:
Non-Hazardous - /

LIT-927 is an orally bioavailable neutraligand that binds to chemokine (C-X-C motif) ligand 12 (CXCL12; Ki = 267 nM in a FRET-based binding assay).{50130} It is selective for inhibiting calcium accumulation induced by CXCL12 over that induced by chemokine (C-C motif) ligand 17 (CCL17), CCL22, CCL5, and CCL2 at 10 µM. It inhibits pulmonary artery smooth muscle cell and pericyte migration in vitro.{52003} LIT-927 (100 mg/kg per day) inhibits increases in serum levels of CXCL12, as well as reduces total pulmonary vascular resistance and remodeling of pulmonary arterioles, in a rat model of pulmonary hypertension induced by monocrotaline (Item No. 16666). It inhibits allergen-induced eosinophil infiltration into the lung by 62% in a mouse model of allergic airway hypereosinophilia when administered at an oral dose of 1,400 µmol/kg.  

 

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Description

A neutraligand of CXCL12 (Ki = 267 nM in a FRET-based binding assay); selective for inhibiting calcium accumulation induced by CXCL12 over that induced by CCL17, CCL22, CCL5, and CCL2 at 10 µM; inhibits increases in serum levels of CXCL12, as well as reduces total pulmonary vascular resistance and remodeling of pulmonary arterioles, in a rat model of monocrotaline-induced pulmonary hypertension at 100 mg/kg per day; inhibits allergen-induced eosinophil infiltration into the lung by 62% in a mouse model of allergic airway hypereosinophilia at 1,400 µmol/kg

Formal name: 4-(4-chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)-2(1H)-pyrimidinone

Synonyms: 

Molecular weight: 328.8

CAS: 2172879-52-4

Purity: ≥98%

Formulation: A solid

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