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Tocris/LY 344864 hydrochloride/2451/50/50 mg

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货号: 2451/50

品牌: Tocris

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Description: Potent, selective 5-HT_1F agonist

Chemical Name: N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide hydrochloride

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent, selective 5-HT_1F receptor agonist (EC₅₀ = 3 nM). Displays > 80-fold selectivity over other 5-HT receptors (K_i values are 0.006, 0.53, 0.55, 0.56, 1.42, 1.70, 3.50, 3.94 and 4.85 μM for 5-HT_1F, 5-HT_1A, 5-HT_1B, 5-HT_1D, 5-HT_1E, 5-HT_2B, 5-HT_2C, 5-HT_2A and 5-HT₇ receptors respectively). Inhibits neurogenic dural inflammation in vivo following i.v. and oral administration.

Licensing Information

Sold under license from Eli Lilly and Company

Compound Libraries

LY 344864 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	387.88
Formula	C₂₁H₂₂N₃OF.HCl
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	1217756-94-9
PubChem ID	56972176
InChI Key	OKUHLSYESBLBCP-PKLMIRHRSA-N
Smiles	Cl[H].CN(C)[C@@H]1CCC2=C(C1)C1=CC(NC(=O)C3=CC=C(F)C=C3)=CC=C1N2

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	38.79	100
	ethanol	1.93	5
	water	19.39	50

Preparing Stock Solutions

The following data is based on the product molecular weight 387.88. 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	2.58 mL	12.89 mL	25.78 mL
5 mM	0.52 mL	2.58 mL	5.16 mL
10 mM	0.26 mL	1.29 mL	2.58 mL
50 mM	0.05 mL	0.26 mL	0.52 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Ramadan et al (2003) 5-HT_1F receptor agonists in acute migraine treatment: a hypothesis. Cephalalgia 23 776 PMID: 14510923

Goadsby and Classey (2003) Evidence for serotonin (5-HT)_1B, 5-HT_1D and 5-HT_1F receptor inhibitory effects on trigeminal neurons with craniovascular input. Neuroscience 122 491 PMID: 14614913

Lee et al (1997) Characterization of LY344864 as a pharmacological tool to study 5-HT_1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Science 61 2117 PMID:

Keywords: LY 344864 hydrochloride, supplier, Potent, selective, 5-HT1F, agonists, Serotonin, Receptors, LY344864, hydrochloride, 5-HT1F, Receptors, 5-HT1F, Receptors, Tocris Bioscience

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