SB269970 HCl (SB-269970A)

Alias: SB269970; GR125743; SB 269970; GR125743; GR-125743; SB-269970; SB269970 HCl
Cat No.:V1019 Purity: ≥98%
SB269970 HCl (SB 269970; GR125743; GR-125743; SB-269970), the hydrochloride salt form of SB-269970, is a novel and potent 5-HT7 receptor antagonist withantianxiety-like effects.
SB269970 HCl (SB-269970A) Chemical Structure CAS No.: 261901-57-9
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 HCl (SB-269970A):

  • SB269970 (SB-269970A)
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Product Description

SB269970 HCl (SB 269970; GR125743; GR-125743; SB-269970), the hydrochloride salt form of SB-269970, is a novel and potent 5-HT7 receptor antagonist with antianxiety-like effects. It shows >50-fold selectivity for 5-HT7 over other receptors and inhibits 5-HT7 with a pKi of 8.3.

Biological Activity I Assay Protocols (From Reference)
Targets
5-HT7 Receptor ( pKi = 8.3 nM )
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. [2]

ln Vivo
SB-269970 (10 mg/kg and 30 mg/kg) blocks the effects of ketamine by 38% (10 mg/kg) and 30% (30 mg/kg), and dramatically reduces the effects of amphetamine by 25 and 27%, respectively. In wild-type mice, SB-269970 significantly lowers amphetamine-induced hyperactivity, while in 5-HT7 knockout mice, it has no effect. When compared to control, systemic administration of SB-269970 (30 mg/kg) significantly reverses the disruption of PPI caused by amphetamines and does not improve PPI on its own.[3] SB-269970 significantly heals the deficits caused by scopolamine, but not by MK-801. MK-801-induced glutamate release in the cortex is normalized by SB-269970, but not dopamine release. In [4] In the rats' Vogel drinking test, the rats' elevated plus-maze test, and the mice's four-plate test, SB-269970 (at one medium dose of 0.5 or 1 mg/kg) exhibits a particular antianxiety-like effect. Furthermore, in mice's forced swimming and tail suspension tests, SB-269970 (at a single medium dose of 5 or 10 mg/kg) exhibits antidepressant-like activity.[5] At 0.3, 1 and 3 μg, SB-269970 displays a less potent anti-conflict effect than diazepam (40 μg); however, at 3 and 10 μg, SB-269970 demonstrated a strong anti-immobility effect similar to imipramine (0.1 μg). [6]
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]. Br J Pharmacol . 2000 Jun;130(3):539-48.

[2]. Br J Pharmacol . 2001 Apr;132(7):1574-80.

[3]. Behav Pharmacol . 2008 Mar;19(2):153-9.

[4]. FASEB J, 2009, 23, Meeting Abstract Supplement, 586.6.

[5]. Neuropharmacology . 2006 Sep;51(3):578-86.

[6]. Eur J Pharmacol . 2006 Dec 28;553(1-3):185-90.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H29CLN2O3S
Molecular Weight
388.95
Exact Mass
352.18
Elemental Analysis
C, 55.58; H, 7.52; Cl, 9.11; N, 7.20; O, 12.34; S, 8.24
CAS #
261901-57-9
Related CAS #
SB-269970; 201038-74-6
Appearance
Solid powder
SMILES
CC1CCN(CC1)CC[C@H]2CCCN2S(=O)(=O)C3=CC=CC(=C3)O.Cl
InChi Key
XQCJOYZLWFNDIO-PKLMIRHRSA-N
InChi Code
InChI=1S/C18H28N2O3S.ClH/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;1H/t16-;/m1./s1
Chemical Name
3-[(2R)-2-[2-(4-methylpiperidin-1-yl)ethyl]pyrrolidin-1-yl]sulfonylphenol;hydrochloride
Synonyms
SB269970; GR125743; SB 269970; GR125743; GR-125743; SB-269970; 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: ~11 mg/mL (~28.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 3: 30% Propylene glycol , 5% Tween 80 , 65% D5W: 30mg/mL


Solubility in Formulation 4: 10 mg/mL (25.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5710 mL 12.8551 mL 25.7102 mL
5 mM 0.5142 mL 2.5710 mL 5.1420 mL
10 mM 0.2571 mL 1.2855 mL 2.5710 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.

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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 HCl
    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 HCl
    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 HCl
    Effect of SB-269970-A on 5-CT-induced hypothermia in guinea-pigs.Br J Pharmacol.2000 Jun;130(3):539-48.
  • SB269970 HCl
    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 HCl
    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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