Tocris/JNJ 10181457 dihydrochloride/4019/10/10 mg-蚂蚁淘生物

Description: H₃ antagonist Chemical Name: 4-[3-[4-[Piperidinyl]but-1-ynyl]benzyl]morpholine dihydrochloride Purity: ≥98% (HPLC) Biological Activity Technical Data Solubility Calculators DatasheetsReferences

Biological Activity

Histamine H₃ receptor antagonist (pK_i values are 8.15 and 8.93 for rat and human H₃ receptors respectively). Increases extracellular norepinephrine and acetylcholine levels in rat frontal cortex but does not stimulate dopamine release. Brain penetrant.

Licensing Information

Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.

Technical Data

M. Wt	385.37
Formula	C₂₀H₂₈N₂O.2HCl
Storage	Desiccate at RT
Purity	≥98% (HPLC)
CAS Number	544707-20-2
PubChem ID	10237424
InChI Key	PAQHERKZFLOHCA-UHFFFAOYSA-N
Smiles	C1(CN2CCOCC2)=CC=CC(C#CCCN3CCCCC3)=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

ethanol	9.63	25
water	38.54	100

Preparing Stock Solutions

The following data is based on the product molecular weight 385.37. 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	2.59 mL	12.97 mL	25.95 mL
5 mM	0.52 mL	2.59 mL	5.19 mL
10 mM	0.26 mL	1.3 mL	2.59 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution. Reconstitution Calculator

Reconstitution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Product Datasheets

Certificate of Analysis / Product Datasheet Safety Datasheet Select another language: English German French Spanish View SDS

References

References are publications that support the products\' biological activity.

Bonaventure et al (2007) Histamine H₃ receptor antagonists: from target identification to drug leads. Biochem.Pharmacol. 73 1084 PMID: 17129577

Esbenshade et al (2008) The histamine H₃ receptor: an attractive target for the treatment of cognitive disorders. Br.J.Pharmacol. 154 1166 PMID: 18469850

Boggs et al (2009) JNJ-10181457, a selective non-imidazole histamine H₃ receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition. Neuropharmacology 56 1131 PMID: 19345233

Keywords: JNJ 10181457 dihydrochloride, supplier, JNJ10181457, dihydrochloride, histamine, h3, receptors, antagonists, brain, penetrant, Histamine, H3, Receptors, Histamine, H3, Receptors, Tocris Bioscience