1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR

LIT-927 

Cat. No.: HY-112709 Purity: 99.66%
Handling Instructions

LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12-TR binding.

For research use only. We do not sell to patients.

LIT-927 Chemical Structure

LIT-927 Chemical Structure

CAS No. : 2172879-52-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
25 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 790 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Technical Information

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  • References

Description

LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12-TR binding.

IC50 & Target

Ki: 267 nM (CXCL12-TR)[1].

In Vitro

LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12-TR binding. 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].

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].

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (38.02 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0418 mL 15.2091 mL 30.4182 mL
5 mM 0.6084 mL 3.0418 mL 6.0837 mL
10 mM 0.3042 mL 1.5209 mL 3.0418 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (3.80 mM); Clear solution

References
Molecular Weight

328.75

Formula

C₁₇H₁₃ClN₂O₃

CAS No.

2172879-52-4

SMILES

ClC1=CC=C(C(C=C(C2=CC=C(O)C(OC)=C2)N3)=NC3=O)C=C1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
LIT-927
Cat. No.:
HY-112709
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LIT-927

Cat. No.: HY-112709