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Tocris/PRE-084 hydrochloride/0589/10/10 mg

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货号: 0589/10

品牌: Tocris

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Description: Highly selective σ₁ agonist

Chemical Name: 2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

High affinity, selective σ₁ agonist (K_i values are 2.2 and 13091 nM for σ₁ and σ₂ receptors respectively). Selective over PCP receptors (IC₅₀ > 100000 nM) and several other receptor systems. Produces antiamnesic and antitussive effects in vivo. Also exhibits protective effects in PC6.3 cells expressing mutant huntingtin by activating NF-κB signaling.

Compound Libraries

PRE-084 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	353.89
Formula	C₁₉H₂₇NO₃.HCl
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	138847-85-5
PubChem ID	11314197
InChI Key	QUJWFJNHTBKCLU-UHFFFAOYSA-N
Smiles	Cl.O=C(OCCN1CCOCC1)C1(CCCCC1)C1=CC=CC=C1

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	26.54	75
	water		25

Preparing Stock Solutions

The following data is based on the product molecular weight 353.89. 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	2.83 mL	14.13 mL	28.26 mL
5 mM	0.57 mL	2.83 mL	5.65 mL
10 mM	0.28 mL	1.41 mL	2.83 mL
50 mM	0.06 mL	0.28 mL	0.57 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Brown et al (2004) Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br.J.Pharmacol. 141 233 PMID: 14691051

Maurice et al (1999) The attenuation of learning impairments induced after exposure to CO or trimethyltin in mice by sigma (σ) receptor ligands involves both σ1 and σ2 sites. Br.J.Pharmacol. 127 335 PMID: 10385231

Su et al (1991) Sigma compounds derived from phencyclidine. Identification of PRE-084, a new selective sigma ligand. J.Pharmacol.Exp.Ther. 259 543 PMID: 1658302

Hyrskyluoto et al (2013) Sigma-1 receptor agonist PRE084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway. Cell Death Dis. 4 e646 PMID: 23703391

Keywords: PRE-084 hydrochloride, supplier, selective, σ1, sigma1, agonists, Receptors, cytoprotective, Sigma1, Receptors, Sigma1, Receptors, Tocris Bioscience

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