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SB 271046(SB-271046A)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB 271046(SB-271046A)图片
CAS NO:209481-20-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)451.99
FormulaC20H22ClN3O3S2
CAS No.209481-20-9(free base);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 40 mg/mL (81.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)1% methylcellulose: ~30 mg/mL
SynonymsSB-271046; SB 271046; SB271046; SB-271046 HCl; SB-271046 hydrochloride
SMILES CodeO=S(C1=C(C)C2=CC(Cl)=CC=C2S1)(NC3=CC=C(OC)C(N4CCNCC4)=C3)=O.[H]Cl
实验参考方法
In Vitro

In vitro activity: SB-271046 also potently displaces [125I]-SB-258585 from rat and pig striatal and human caudate putamen membranes with pKis of 9.02, 8.55 and 8.81, respectively. SB-271046 competitively antagonizes 5-HT-induced stimulation of adenylyl cyclase activity with a pA2 of 8.71. SB-271046 is found to be a competitive antagonist with a pA2 of 8.7 in the functional adenylyl cyclase assay which is in good agreement with its binding affinity. SB-271046 demonstrates no significant inhibitory activity at the major human P450 enzymes.


Kinase Assay: SB271046 Hcl is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9. IC50 Value: 8.9(pKi). SB 271046 hydrochloride is a sulfonamidal benzothiophene derivative that has been shown to act as a selective 5-HT6 antagonist with pKi values of 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27 and < 4.99 for 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E respectively, and is> 200-fold selective over 55 other receptors, enzymes and ion channels.

In VivoSB-271046 produces an increase in seizure threshold over a wide-dose range in the rat maximal electroshock seizure threshold (MEST) test, with a minimum effective dose of 0.1 mg/kg p.o. and maximum effect at 4 hours post-dose. The level of anticonvulsant activity achieves correlated well with the blood concentrations of SB-271046 (EC50 of 0.16 μM) and brain concentrations of 0.01 μM–0.04 μM at Cmax. SB-271046 is moderately brain penetrant (10%), subject to low blood clearance (7.7 mL/min/kg) with a good half-life in rats (4.8 hours), and has excellent oral bioavailability (>80%). SB-271046 produces 3-fold and 2-fold increases in extracellular glutamate levels in both frontal cortex and dorsal hippocampus of rats, respectively, which may be used for the treatment of cognitive and memory dysfunction. SB-271046 (20 mg/kg, orally gavage) 30 min prior to training Wistar rats, is found to reverse significantly the amnesia produced by administering scopolamine (0.8 mg/kg, i.p.) in the 6 hours post-training period. SB-271046 progressively and significantly decreases platform swim angle and escape latencies over the five sequential trials on four consecutive daily sessions compared to vehicle-treated controls in aged rats. SB-271046 also improves task recall as measured by significant increases in the searching of the target quadrant on post-training days 1 and 3. SB-271046 (10 mg/kg, s.c.) produces a significant, tetrodotoxin-dependent, increase in extracellular levels of both glutamate and aspartate within the frontal cortex of rats, reaching maximum values of 375.4% and 215.3% of preinjection values, respectively.
Animal modelMale Sprague Dawley rats
Formulation & DosageDissolved in 1% methyl cellulose in water; 30 mg/kg; Oral gavage
ReferencesBr J Pharmacol. 2000 Aug;130(7):1606-12; J Med Chem. 1999 Jan 28;42(2):202-5.