Chemical Name: 4-(4-Chlorophenyl)-4-hydroxy-α,α-diphenyl-1-piperidinepentanenitrile hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Selective CCR1 receptor antagonist (Ki values are 0.04, > 10, > 10 and > 10 nM for CCR1, CCR5, CXCR2 and CXCR4 receptors respectively). Inhibits MIP-1α-induced intracellular calcium mobilization (IC50 = 2.5 μM). Also a full inverse agonist at US28, a HCMV-encoded chemokine receptor.
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
48.15
100
ethanol
24.07
50
Preparing Stock Solutions
The following data is based on the product molecular weight 481.46. 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.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.08 mL
10.39 mL
20.77 mL
5 mM
0.42 mL
2.08 mL
4.15 mL
10 mM
0.21 mL
1.04 mL
2.08 mL
50 mM
0.04 mL
0.21 mL
0.42 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Hesselgesseret al (1998) Identification and characterisation of small molecule functional antagonists of the CCR1 chemokine receptor. J.Biol.Chem. 273 15687 PMID: 9624164
Nget al (1999) Discovery of a novel non-peptide CCR1 receptor antagonists. J.Med.Chem. 42 4680 PMID: 10579830
Casarosaet al (2003) Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G-protein-coupled receptor. J.Biol.Chem. 278 5172 PMID: 12456673