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LIT927

Catalog No. T5207 CAS 2172879-52-4

Synonyms: LIT 927, LIT-927

LIT927 (LIT-927) is an orally active CXCL12 neutraligand (Ki: 267 nM for CXCL12 binding to CXCR4).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

LIT927, CAS 2172879-52-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 45.00
5 mg	In stock	$ 70.00
10 mg	In stock	$ 112.00
25 mg	In stock	$ 216.00
50 mg	In stock	$ 347.00
100 mg	In stock	$ 582.00
500 mg	In stock	$ 1,270.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.73%

Purity: 99.57%

Biological Description

Chemical Properties

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Description	LIT927 (LIT-927) is an orally active CXCL12 neutraligand (Ki: 267 nM for CXCL12 binding to CXCR4).
Targets&IC50	CXCL12:267 nM (Ki)
In vitro	LIT-927 at 10 μM is able to inhibit the increase in intracellular calcium concentration in EGFP-CXCR4+ HEK cells in response to CXCL12, while it has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CCR4+ HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or CCL2 on EGFPCCR2+ HEK cells [1].
In vivo	LIT-927 (350 μmol/kg) inhibited eosinophil infiltration by 54% and 55%. LIT-927 did not exhibit any side effects. In the same murine model of hypereosinophilia, LIT-927 (1400 μmol/kg, P.O.) shows a large and statistically reliable inhibition of eosinophil recruitment (62% inhibition) [1].
Cell Research	HEK EGFP-CXCR4-expressing cells were washed with phosphate-buffered saline (PBS) and detached in PBS-EDTA (5 mM) for 2 min at room temperature. Then cells were carefully resuspended in complete growth medium, pelleted by centrifugation at 320 × g for 5 min, and resuspended in HEPES buffer (137.5 mM NaCl, 6 mM KCl, 1.25 mM CaCl2, 1.25 mM MgCl2, 0.4 mM NaH2PO4, 5.6 mM glucose, 10 mM HEPES (pH 7.4) containing 0.1% BSA. Cells were used at a concentration of 10^6 cells/mL, then the cell suspension (1 mL) was transferred into a quartz cuvette. Time-based recordings of the fluorescence emitted at 510 nm (excitation at 470 nm) were performed at 21 °C using a Fluorolog 3 spectrofluorometer. Fluorescence binding measurements were initiated by adding at t = 150 s, 100 nM CXCL12-Texas Red (TR) to the 1 mL cell suspension. Binding of CXCL12-TR to EGFP-labeled CXCR4 was detected as a reversible decline of emission at 510 nm due to energy transfer from excited EGFP to TR. In the "neutraligand protocol", CXCL12-TR was preincubated for 1 h at room temperature with DMSO or various concentrations of each test compound. Then the premix was added (at t = 150 s), and fluorescence was recorded until equilibrium was reached (300 s). In the "antagonist protocol", DMSO or various concentrations of each test compound were added to EGFP-CXCR4-expressing cells at t = 50 s. Then CXCL12-Texas Red (100 nM) was added at t = 150 s, and fluorescence was recorded until equilibrium was reached (300 s). Dose-response curves of inhibition of CXCL12-TR binding were performed, and the inhibitory constants (Ki) of the different compounds were determined. T134 (20 μM), the CXCR4 receptor antagonist, was used as a control in both "neutraligand" and "antagonist" protocols.
Animal Research	The activity of each compound was assessed in vivo in an 8 day model of allergic eosinophilic airway inflammation as described previously. Briefly, 9 week-old male Balb/c mice were sensitized by intraperitoneal injection of 50 μg of ovalbumin adsorbed on 2 mg of aluminum hydroxide in 0.1 mL of saline on days 0, 1, and 2. Mice were challenged intranasally [10 μg of OVA in 25 μL of saline (12.5 μL/nostril)] on days 5, 6, and 7. Control mice received intranasal administration of saline alone. Intranasal administrations were performed under anesthesia with intraperitoneal injection of ketamine (50 mg/kg) and xylazine (3.33 mg/kg). Food and water were supplied ad libitum. Two hours before each OVA or saline challenge, compounds in PBS/Cdx were administered intranasally (12.5 μL/nostril), intraperitoneally, or per os as indicated in the figure legends. Bronchoalveolar lavage (BAL) was performed 24 h after the last OVA or saline challenge as described. Mice were deeply anesthetized by intraperitoneal injection of ketamine (150 mg/kg) and xylazine (10 mg/kg). A plastic cannula was inserted into the trachea, and airways were lavaged by 10 instillations of 0.5 mL of ice-cold saline supplemented with 2.6 mM EDTA (saline-EDTA). BAL fluids were centrifuged (300g, 5 min, 4 °C) to pellet cells, and erythrocytes were lysed by hypotonic shock. Cells were resuspended in 500 μL of icecold saline-EDTA, and total cell counts were determined on a hemocytometer. Differential cell counts were assessed on cytological preparations spanning 250 000 cells/mL in ice-cold saline?EDTA, stained with Diff-Quick with counts of at least 400 cells. Counts were expressed as absolute cell numbers or percentage of inhibition of eosinophil recruitment.

Synonyms	LIT 927, LIT-927
Molecular Weight	328.75
Formula	C17H13ClN2O3
CAS No.	2172879-52-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: Insoluble

DMSO: 25 mg/mL (76.05 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library GPCR Compound Library Bioactive Compounds Library Max Cytokine Inhibitor Library NO PAINS Compound Library Orally Active Compound Library Stem Cell Differentiation Compound Library Autophagy Compound Library Nonsteroidal Anti-Inflammatory Compound Library Immunology/Inflammation Compound Library

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Keywords

LIT927 2172879-52-4 Autophagy GPCR/G Protein Immunology/Inflammation CXCR LIT 927 LIT-927 inhibitor inhibit

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