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LIT-927

Cat. No. M20649
LIT-927 Structure
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Biological Activity

LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma.

Chemical Information
Molecular Weight 328.75
Formula C17H13ClN2O3
CAS Number 2172879-52-4
Solubility (25°C) DMSO 66 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rebecca Bignold, et al. Respir Res. Chemokine CXCL12 drives pericyte accumulation and airway remodeling in allergic airway disease

[2] Qisheng Xiong, et al. J Biomed Mater Res B Appl Biomater. Engineer a pre-metastatic niched microenvironment to attract breast cancer cells by utilizing a 3D printed polycaprolactone/nano-hydroxyapatite osteogenic scaffold - An in vitro model system for proof of concept

[3] Nicolas Schall, et al. Front Pharmacol. A Selective Neutraligand for CXCL12/SDF-1α With Beneficial Regulatory Functions in MRL/Lpr Lupus Prone Mice

[4] Jennifer Bordenave, et al. Cardiovasc Res. Neutralization of CXCL12 attenuates established pulmonary hypertension in rats

[5] Pierre Regenass, et al. J Med Chem. Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia

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