BX 471

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Cat.No. 3496 - BX 471 | C21H24ClFN4O3 | CAS No. 217645-70-0
Description: Potent, selective CCR1 antagonist
Chemical Name: (2R)-1-[[2-[(Aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methylpiperazine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1). Exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4. Inhibits MIP-α/CCL3-induced intracellular Ca2+ mobilization. Orally active; effectively reduces disease severity in a rat model of multiple sclerosis. Decreases renal fibrosis in a mouse model of obstructive nephropathy.

Compound Libraries

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Technical Data

M. Wt 434.89
Formula C21H24ClFN4O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 217645-70-0
PubChem ID 512282
InChI Key XQYASZNUFDVMFH-CQSZACIVSA-N
Smiles FC1=CC=C(CN2C[C@@H](C)N(C(COC3=CC=C(Cl)C=C3NC(N)=O)=O)CC2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.49 100
ethanol 21.74 50

Preparing Stock Solutions

The following data is based on the product molecular weight 434.89. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.3 mL 11.5 mL 22.99 mL
5 mM 0.46 mL 2.3 mL 4.6 mL
10 mM 0.23 mL 1.15 mL 2.3 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Liang (2000) Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J.Biol.Chem. 275 19000 PMID: 10748002

Anders (2002) A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J.Clin.Invest. 109 251 PMID: 11805137

Furuichi et al (2008) Chemokine receptor CCR1 regulates inflammatory cell infiltration after renal ischemia-reperfusion injury. J.Immunol. 181 8670 PMID: 19050287


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Keywords: selective chemokine receptor antagonists CCR1 BX471 multiple sclerosis renal fibrosis leukocyte recruitment Rantes Chemokine CC Receptors

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