A 331440 dihydrochloride

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Cat.No. 4697 - A 331440 dihydrochloride | CAS No. 1049740-32-0
Description: Selective H3 antagonist
Chemical Name: 4'-[3-[(3R)-3-(Dimethylamino)-1-pyrrolidinyl]propoxy]-[1,1'-biphenyl]-4-carbonitrile dihydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

High affinity histamine H3 receptor antagonist (Ki values are 21.7 and 22.7 nM for rat and human H3 receptors, respectively). Exhibits selectivity for human H3 over H1, H2 and H4 receptors (Ki values are 2940, 14400 and >10000 nM respectively). Shown to reduce weight in a diet-induced obesity model.

Technical Data

M. Wt 422.39
Formula C22H27N3O.2HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1049740-32-0
PubChem ID 16078942
InChI Key XFPYVTSGYYMTFS-GHVWMZMZSA-N
Smiles CN(C)[C@H](CC3)CN3CCCOC1=CC=C(C2=CC=C(C#N)C=C2)C=C1.Cl.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
water 42.24 100
DMSO 8.45 20

Preparing Stock Solutions

The following data is based on the product molecular weight 422.39. 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 2.37 mL 11.84 mL 23.67 mL
5 mM 0.47 mL 2.37 mL 4.73 mL
10 mM 0.24 mL 1.18 mL 2.37 mL
50 mM 0.05 mL 0.24 mL 0.47 mL

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References

References are publications that support the biological activity of the product.

Hancock et al (2004) Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist. Eur.J.Pharmacol. 487 183 PMID: 15033391

Hancock et al (2004) In vitro optimization of structure activity relationships by analogues of A-331440 combining radioligand receptor binding assays and micronucleus assays of potential antiobesity histamine H3 receptor antagonists. Basic Clin.Pharmacol.Toxicol. 95 144 PMID: 15447739


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