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SB-269970 hydrochloride

Catalog No. T6655   CAS 261901-57-9
Synonyms: SB-269970A, SB269970 HCl

SB-269970 hydrochloride (SB-269970A) , a hydrochloride salt form of SB-269970, is a 5-HT7 receptor antagonist (pKi of 8.3) and exhibits <50-fold selectivity against other receptors.

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SB-269970 hydrochloride Chemical Structure
SB-269970 hydrochloride, CAS 261901-57-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 50.00
5 mg In stock $ 68.00
10 mg In stock $ 125.00
25 mg In stock $ 270.00
50 mg In stock $ 473.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 98.45%
ee: 100%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SB-269970 hydrochloride (SB-269970A) , a hydrochloride salt form of SB-269970, is a 5-HT7 receptor antagonist (pKi of 8.3) and exhibits >50-fold selectivity against other receptors.
Targets&IC50 5-HT7:8.3(pKi)
In vitro SB-269970 inhibits 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes. SB-269970 (0.03 μM, 0.1 μM, 0.3 μM and 1 μM) produces a concentration-related rightward-shift of the 5-CT concentration-response curve with no significant alteration in the maximal response to 5-CT. [1] SB-269970 (1 μM) has any effect on 5-HT efflux when superfused alone. [2]
In vivo SB-269970 (10 mg/kg and 30 mg/kg) significantly reduces the effects of amphetamine by 25 and 27%, respectively, and blocks the effects of ketamine by 38% (10 mg/kg) and 30% (30 mg/kg). SB-269970 significantly reduces amphetamine-induced hyperactivity in wild-type mice and is without effects in 5-HT7 knockout mice. Systemic administration of SB-269970 (30 mg/kg) significantly reverses amphetamine disruption of PPI and did not enhance PPI by itself compared to control. [3] SB-269970 significantly reverses the deficits induced by MK-801, but not by scopolamine. SB-269970 normalizes MK-801-induced glutamate but not dopamine release in the cortex. [4] SB-269970 (in one medium dose of 0.5 or 1 mg/kg) exerts a specific antianxiety-like effect in the Vogel drinking test in rats, in the elevated plus-maze test in rats and in the four-plate test in mice. Moreover, SB-269970 (in one medium dose of 5 or 10 mg/kg) reveals antidepressant-like activity in the forced swimming and the tail suspension tests in mice. [5] SB-269970 at doses of 0.3, 1 and 3 μg exhibits an anticonflict effect which is weaker than that of diazepam (40 μg), whereas SB-269970 at doses of 3 and 10 μg had marked anti-immobility action comparable to that of imipramine (0.1 μg). [6]
Synonyms SB-269970A, SB269970 HCl
Molecular Weight 388.95
Formula C18H28N2O3S·HCl
CAS No. 261901-57-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 7.8 mg/mL (20 mM)

DMSO: 38.9 mg/mL (100 mM)

TargetMolReferences and Literature

1. Hagan JJ, et al. Br J Pharmacol, 2000, 130(3), 539-548. 2. Roberts C, et al. Br J Pharmacol, 2001, 132(7), 1574-1580. 3. Galici R, et al. Behav Pharmacol, 2008, 19(2), 153-159. 4. Galici R, et al. FASEB J, 2009, 23, Meeting Abstract Supplement, 586.6. 5. Wesołowska A, et al. Neuropharmacology. 2006 Sep;51(3):578-86.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Bioactive Compound Library Serotonin Receptor-Targeted Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max

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Keywords

SB-269970 hydrochloride 261901-57-9 GPCR/G Protein Neuroscience 5-HT Receptor SB 269970 5-hydroxytryptamine Receptor SB 269970 Hydrochloride SB269970 hydrochloride SB 269970 hydrochloride SB269970 SB-269970A Inhibitor SB-269970 Hydrochloride SB269970 HCl SB269970 Hydrochloride SB-269970 inhibit Serotonin Receptor inhibitor

 

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