SB269970 (SB-269970A)

Alias: SB269970; SB 269970; SB-269970; GR125743; GR-125743; SB269970 HCl
Cat No.:V2619 Purity: ≥98%
SB269970 (SB-269970A)is a novel and potent 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.
SB269970 (SB-269970A) Chemical Structure CAS No.: 201038-74-6
Product category: 5-HT Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of SB269970 (SB-269970A):

  • SB269970 HCl (SB-269970A)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SB269970 (SB-269970A) is a novel and potent 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors. SB269970 functions as a 5-HT7 receptor selective antagonist that exhibits at least a 100-fold selectivity against 5-HT7 across a range of receptors and enzymes. Moreover, SB269970 suppresses the 5-CT-stimulated adenylyl cyclase activity in both the guinea-pig hippocampal (pKB of 8.3) and 5-HT7(a)/HEK293 (pA2 of 8.5) membranes.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT7 Receptor ( pKi = 8.3 )
ln Vitro

In vitro activity: SB-269970 inhibits 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes. The concentration-response curve of 5-CT shows a concentration-related rightward shift when SB-269970 (0.03 μM, 0.1 μM, 0.3 μM, and 1 μM) is used, but the maximal response to 5-CT is not significantly changed. When superfused alone, SB-269970 (1 μM) has no effect on 5-HT efflux.

ln Vivo
SB-269970 (3–30 mg/kg; intraperitoneal; once) dramatically inhibits the hyperactivity caused by amphetamine and ketamine[2].
Enzyme Assay
SB269970 an antagonist of the 5-HT7 receptor with pKi of 8.3, exhibits >50-fold selectivity against other receptors.
Animal Protocol
Dissolved in saline; 10 mg/kg, 30 mg/kg; i.p.injection
C57BL6/J mice
References

[1]. Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist. Br J Pharmacol. 2000 Jun;130(3):539-48.

[2]. The effect of SB-269970, a 5-HT(7) receptor antagonist, on 5-HT release from serotonergic terminals and cell bodies. Br J Pharmacol. 2001 Apr;132(7):1574-80.

[3]. Effects of the selective 5-HT7 receptor antagonist SB-269970 and amisulpride on ketamine-induced schizophrenia-like deficits in rats. PLoS One. 2013 Jun 11;8(6):e66695.

[4]. The serotonin 5-HT7 receptor agonist LP-44 microinjected into the dorsal raphe nucleus suppresses REM sleep in the rat. Behav Brain Res. 2008 Aug 22;191(2):184-9.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H28N2O3S
Molecular Weight
352.49
Exact Mass
352.18
Elemental Analysis
C, 61.33; H, 8.01; N, 7.95; O, 13.62; S, 9.10
CAS #
201038-74-6
Related CAS #
SB-269970 hydrochloride; 261901-57-9
Appearance
Solid powder
SMILES
CC1CCN(CC1)CC[C@H]2CCCN2S(=O)(=O)C3=CC=CC(=C3)O
InChi Key
HWKROQUZSKPIKQ-MRXNPFEDSA-N
InChi Code
InChI=1S/C18H28N2O3S/c1-15-7-11-19(12-8-15)13-9-16-4-3-10-20(16)24(22,23)18-6-2-5-17(21)14-18/h2,5-6,14-16,21H,3-4,7-13H2,1H3/t16-/m1/s1
Chemical Name
3-[(2R)-2-[2-(4-methylpiperidin-1-yl)ethyl]pyrrolidin-1-yl]sulfonylphenol
Synonyms
SB269970; SB 269970; SB-269970; GR125743; GR-125743; SB269970 HCl
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
30%propylene glycol+ 5%Tween 80+ 65%D5W: 30.0mg/ml (77.13mM) (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8370 mL 14.1848 mL 28.3696 mL
5 mM 0.5674 mL 2.8370 mL 5.6739 mL
10 mM 0.2837 mL 1.4185 mL 2.8370 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • SB269970
    Stimulation of adenylyl cyclase activity in human 5-HT7/HEK293 membranes by 5-CT alone and in the presence of SB-269970-A (0.03, 0.1, 0.3 and 1 μM).Br J Pharmacol.2000 Jun;130(3):539-48.
  • SB269970
    Stimulation of adenylyl cyclase activity in guinea-pig hippocampal membranes by 5-CT alone and in the presence of SB-269970-A (0.3 μM).Br J Pharmacol.2000 Jun;130(3):539-48.

  • SB269970
    Effect of SB-269970-A on 5-CT-induced hypothermia in guinea-pigs.Br J Pharmacol.2000 Jun;130(3):539-48.
  • SB269970
    Time course of the effects of SB-269970-A on 5-CT-induced hypothermia in guinea-pigs.Br J Pharmacol.2000 Jun;130(3):539-48.
  • SB269970
    Effect of SB-269970-A on sleep stage distribution during the normal sleep phase.Br J Pharmacol.2000 Jun;130(3):539-48.
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