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Submit ReviewBX 471
Description: Potent, selective CCR1 antagonist
Alternative Names: ZK-811752
Chemical Name: (2R)-1-[[2-[(Aminocarbonyl)amino]-4-chlorophenoxy]acetyl]-4-[(4-fluorophenyl)methyl]-2-methylpiperazine
Purity: ≥98% (HPLC)
Biological Activity for BX 471
BX 471 is a 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 for BX 471
BX 471 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for BX 471
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for BX 471
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.49 | 100 | |
| ethanol | 21.74 | 50 |
Preparing Stock Solutions for BX 471
The following data is based on the product molecular weight 434.89. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 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 for BX 471
References for BX 471
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for BX 471, please let us know.
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Citations for BX 471
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Literature in this Area
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