SB269970 HCl

Catalog No.S2849

SB269970 HCl Chemical Structure

Molecular Weight(MW): 388.95

SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.

Size Price Stock Quantity  
In DMSO USD 220 In stock
USD 170 In stock
USD 670 In stock
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1 Customer Review

  • Cells transfected with 5-HT7A receptor, were incubated with agonist with or without antagonist, or antagonist with 1 μM agonist. Three independent experiments were performed in triplicate.

    Sci Rep, 2015, 5:8060.. SB269970 HCl purchased from Selleck.

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Biological Activity

Description SB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors.
Features A hydrochloride salt form of SB-269970 which is a potent 5-HT 7 receptor antagonist.
Targets
5-HT7 [1]
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]

Protocol

Animal Research:[4]
+ Expand
  • Animal Models: C57BL6/J mice
  • Formulation: Dissolved in saline
  • Dosages: 10 mg/kg, 30 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 11 mg/mL (28.28 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 388.95
Formula

C18H28N2O3S.HCl

CAS No. 261901-57-9
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID