SB-200646 HCl
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MedKoo CAT#: 462281

CAS#: 143797-62-0

Description: SB-200646 HCl is a dual antagonist of the serotonin (5-HT) receptor subtypes 5-HT2C and 5-HT2B.


Chemical Structure

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SB-200646 HCl
CAS# 143797-62-0

Theoretical Analysis

MedKoo Cat#: 462281
Name: SB-200646 HCl
CAS#: 143797-62-0
Chemical Formula: C15H15ClN4O
Exact Mass: 0.00
Molecular Weight: 302.760
Elemental Analysis: C, 59.51; H, 4.99; Cl, 11.71; N, 18.51; O, 5.28

Price and Availability

Size Price Availability Quantity
1mg USD 205 2 Weeks
5mg USD 384 2 Weeks
10mg USD 625 2 Weeks
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Synonym: SB-200646 hydrochloride; SB200646 hydrochloride; SB 200646 hydrochloride; SB-200646 HCl; SB200646 HCl; SB 200646 HCl

IUPAC/Chemical Name: N-(1-methyl-1H-indol-5-yl)-N′-3-pyridinyl-urea, monohydrochloride

InChi Key: IGRYPUQJEDJLHC-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H14N4O.ClH/c1-19-8-6-11-9-12(4-5-14(11)19)17-15(20)18-13-3-2-7-16-10-13;/h2-10H,1H3,(H2,17,18,20);1H

SMILES Code: O=C(NC1=CC(C=CN2C)=C2C=C1)NC3=CC=CN=C3.Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: SB-200646 is a dual antagonist of 5-HT receptor subtypes 5-HT2C (Ki = 125 nM in isolated rat cortex) and 5-HT2B (pA2 = 7.5 in rat stomach fundus preparations). It is selective for 5-HT2C and 5-HT2B over 5-HT1A, 5-HT2A, 5-HT1D, 5-HT3, benzodiazepine, GABAA, α1-, α2A-, α2B-, β1-, and β2-adrenergic, dopamine D1 and D2, and histamine H1 receptors (Kis = >10 µM for all).
In vitro activity: To be determined
In vivo activity: Acute and chronic administration of SB-200646 HCl resulted in various changes in the firing rate, bursting activity, and number of spontaneously active dopamine neurons in the substantia nigra pars compacts and ventral tegmental area of anesthetized rats. Specifically, the administration of SB-200646 HCl led to alterations in firing patterns and neuronal activity resembling those associated with atypical antipsychotic drugs. Reference: Synapse. 2006 Jun 15;59(8):502-12. https://pubmed.ncbi.nlm.nih.gov/16565966/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 250.0 825.74

Preparing Stock Solutions

The following data is based on the product molecular weight 302.76 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Blackburn TP, Suzuki K, Ashby CR Jr. The acute and chronic administration of the 5-HT(2B/2C) receptor antagonist SB-200646A significantly alters the activity of spontaneously active midbrain dopamine neurons in the rat: An in vivo extracellular single cell study. Synapse. 2006 Jun 15;59(8):502-12. doi: 10.1002/syn.20263. PMID: 16565966. 2. Meneses A. Involvement of 5-HT(2A/2B/2C) receptors on memory formation: simple agonism, antagonism, or inverse agonism? Cell Mol Neurobiol. 2002 Dec;22(5-6):675-88. doi: 10.1023/a:1021800822997. PMID: 12585687.
In vitro protocol: To be determined
In vivo protocol: 1. Blackburn TP, Suzuki K, Ashby CR Jr. The acute and chronic administration of the 5-HT(2B/2C) receptor antagonist SB-200646A significantly alters the activity of spontaneously active midbrain dopamine neurons in the rat: An in vivo extracellular single cell study. Synapse. 2006 Jun 15;59(8):502-12. doi: 10.1002/syn.20263. PMID: 16565966. 2. Meneses A. Involvement of 5-HT(2A/2B/2C) receptors on memory formation: simple agonism, antagonism, or inverse agonism? Cell Mol Neurobiol. 2002 Dec;22(5-6):675-88. doi: 10.1023/a:1021800822997. PMID: 12585687.

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1: Kennett, G.A., Wood, M.D., Glen, A., et al. In vivo properties of SB 200646A, a 5-HT2C/2B receptor antagonist. Br. J. Pharmacol. 111(3), 797-802 (1994).