W 54011

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Cat.No. 5455 - W 54011 | C30H36N2O2.HCl | CAS No. 405098-33-1
Description: High affinity C5a receptor antagonist
Chemical Name: N-[[4-(Dimethylamino)phenyl]methyl]-1,2,3,4-tetrahydro-7-methoxy-N-[4-(1-methylethyl)phenyl]-1-naphthalenecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

High affinity C5a receptor antagonist (Ki = 2.2 nM). Inhibits C5a-induced generation of reactive superoxide species, chemotaxis and intracellular Ca2+ mobilization in human neutrophils (IC50 values are 1.6, 2.7 and 3.1 nM, respectively).

Compound Libraries

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Technical Data

M. Wt 493.08
Formula C30H36N2O2.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 405098-33-1
PubChem ID 5311121
InChI Key UKBJWRMNGCDKNL-UHFFFAOYSA-N
Smiles CC(C)C1=CC=C(N(CC2=CC=C(N(C)C)C=C2)C(C3C(C=C(OC)C=C4)=C4CCC3)=O)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 24.65 50
ethanol 4.93 10mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 493.08. 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 2.03 mL 10.14 mL 20.28 mL
5 mM 0.41 mL 2.03 mL 4.06 mL
10 mM 0.2 mL 1.01 mL 2.03 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Sumichika et al (2002) Identification of a potent and orally active non-peptide C5a receptor antagonist. J.Biol.Chem. 277 49403 PMID: 2384495

Monk et al (2007) Function, structure and therapeutic potential of complement C5a receptors. Br.J.Pharmacol. 152 429 PMID: 17603557

Cho et al (2014) Autocrine effects of tumor-derived complement. Cell Rep. 6 1085 PMID: 24613353


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Keywords: W 54011, supplier, W54011, high, affinity, C5a, receptors, antagonists, antagonism, neutrophils, complement, Complement, Complement, Tocris Bioscience

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