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Tocris/SB 243213 dihydrochloride/3527/10/10 mg

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货号: 3527/10

品牌: Tocris

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Description: Selective 5-HT_2C inverse agonist

Chemical Name: 2,3-Dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-1H-Indole-1-carboxamide dihydrochloride

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective 5-HT_2C inverse agonist (pK_b = 9.8). Displays selectivity over other 5-HT₂ subtypes (pK_i values are 6.8, 7.0 and 9.0 for 5-HT_2A, 5-HT_2B and 5-HT_2C respectively); also exhibits >100-fold selectivity over 50 other receptors, ion channels and enzymes. Displays anxiolytic activity in rat models.

Compound Libraries

SB 243213 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	501.33
Formula	C₂₂H₁₉F₃N₄O₂.2HCl
Storage	Store at +4°C
Purity	≥99% (HPLC)
CAS Number	200940-23-4
PubChem ID	90488853
InChI Key	UKMTYUXWLKQDNT-UHFFFAOYSA-N
Smiles	O=C(N3C(C=C(C(F)(F)F)C(C)=C4)=C4CC3)NC(C=C2)=CN=C2OC1=CC=CN=C1C.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
Solubility	DMSO	25.07	50

Preparing Stock Solutions

The following data is based on the product molecular weight 501.33. 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	1.99 mL	9.97 mL	19.95 mL
5 mM	0.4 mL	1.99 mL	3.99 mL
10 mM	0.2 mL	1 mL	1.99 mL
50 mM	0.04 mL	0.2 mL	0.4 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Bromidge et al (2000) Biarylcarbamoylindolines are novel and selective 5-HT_2C receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic a J.Med.Chem. 43 1123 PMID: 10737744

Wood et al (2001) SB-243213; a selective 5-HT_2C receptor inverse agonist with improved anxiolytic profile: lack of tolderance and withdrawal anxiety. Neuropharmacology 41 186 PMID: 11489455

Berg et al (2006) Differential effects of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxyl]-5-pyridyl]carbamoyl]-6-trifluoromethylindone (SB 243213) on 5-hydroxytryptamine_2C receptor-mediated responses. J.Pharmacol.Exp.Ther. 319 260 PMID: 16807362

Keywords: SB 243213 dihydrochloride, supplier, SB243213, dihydrochloride, selective, 5-ht3, inverse, agonists, serotonergics, 5-HT2C, Receptors, 5-HT2C, Receptors, Tocris Bioscience

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