
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.
Technical Data
M. Wt | 481.46 |
Formula | C28H29ClN2O.HCl |
Storage | Desiccate at +4°C |
Purity | ≥99% (HPLC) |
CAS Number | 1216540-18-9 |
PubChem ID | 56972186 |
InChI Key | SSZWNUGWOGONQJ-UHFFFAOYSA-N |
Smiles | ClC1=CC=C(C2(O)CCN(CCCC(C4=CC=CC=C4)(C#N)C3=CC=CC=C3)CC2)C=C1.Cl |
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
References
References are publications that support the products' biological activity.
Hesselgesser et al (1998) Identification and characterisation of small molecule functional antagonists of the CCR1 chemokine receptor. J.Biol.Chem. 273 15687 PMID: 9624164
Ng et al (1999) Discovery of a novel non-peptide CCR1 receptor antagonists. J.Med.Chem. 42 4680 PMID: 10579830
Casarosa et 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
Keywords: BX 513 hydrochloride, supplier, Selective, CCR1, antagonists, chemokine, Receptors, BX513, hydrochloride, VUF2274, Rantes, VUF, 2274, Chemokine, CC, Receptors, Chemokine, CC, Receptors, Tocris Bioscience