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SB-242084 (hydrochloride) (CAS 1049747-87-6) LS-H68

5-HT2C receptor agonist
LS-H68-1 / 1 mg / $175
LS-H68-5 / 5 mg / $225
LS-H68-10 / 10 mg / $245
USA Shipment Only
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Description: Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT2C receptor (pKi = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors. In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties. SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT2C receptor agonists and neurotransmitter receptor interactions in mice. H68_ChemicalStructureImage.png
6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole-1-carboxamide, dihydrochloride
 
biochemical, chemical, agonist
LS-H68
1049747-87-6
C21H19ClN4O2 • 2HCl
≥98%
A crystalline solid
 
CC1=NC=CC=C1OC(N=C2)=CC=C2NC(N3CCC4=C3C=C(Cl)C(C)=C4)=O.Cl.Cl
InChI=1S/C21H19ClN4O2.2ClH/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2;;/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27);2*1H
GCMNSEILNIPNSX-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: HTR2C / 5-HT2C Receptor related products

Usage Information

SB-242084 (hydrochloride) is supplied as a crystalline solid. A stock solution may be made by dissolving the SB-242084 (hydrochloride) in the solvent of choice. SB-242084 (hydrochloride) is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of SB-242084 (hydrochloride) in ethanol is approximately 1 mg/ml and approximately 30 mg/ml in DMSO and DMF. Further dilutions of the stock solution into aqueous buffers or isotonic saline should be made prior to performing biological experiments. Ensure that the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. Organic solvent-free aqueous solutions of SB-242084 (hydrochloride) can be prepared by directly dissolving the crystalline compound in aqueous buffers. The solubility of SB-242084 (hydrochloride) in PBS, pH 7.2, is approximately 10 mg/ml. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Kennett, G.A., Wood, M.D., Bright, F., et al. Neuropharmacology 36(4/5), 609-620 (1997).
  2. Bromidge, S.M., Duckworth, M., Forbes, I.T., et al. J. Med. Chem. 40, 3494-3496 (1997).
  3. Fletcher, P.J., Tampakeras, M., Sinyard, J., et al. Neuropharmacology 57, 259-267 (2009).
  4. Fletcher, P.J., Sinyard, J., and Higgins, G.A. Psychopharmacology 187, 515-525 (2006).
  5. Dalton, G.L., Lee, M.D., Kennett, G.A., et al. Psychopharmacology 185, 45-47 (2006).

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