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安全信息

S4326

Sigma-Aldrich

SB-277011-A hydrochloride hydrate

≥98% (HPLC)

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100 μL
¥1,522.27

¥1,522.27

目录价¥5,074.24节省 70%

国内现货,预计发货时间2025年4月25日详情


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100 μL
¥1,522.27

About This Item

经验公式(希尔记法):
C28H30N4O · HCl · xH2O
分子量:
475.02 (anhydrous basis)
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

¥1,522.27

目录价¥5,074.24节省 70%

国内现货,预计发货时间2025年4月25日详情


获取大包装报价

质量水平

方案

≥98% (HPLC)

表单

powder

储存条件

protect from light

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear (warmed)

创始人

GlaxoSmithKline

储存温度

2-8°C

SMILES字符串

O.Cl.O=C(N[C@@H]1CC[C@H](CC1)CCN2CCc3cc(ccc3C2)C#N)c4ccnc5ccccc45

InChI

1S/C28H30N4O.ClH.H2O/c29-18-21-5-8-23-19-32(16-13-22(23)17-21)15-12-20-6-9-24(10-7-20)31-28(33)26-11-14-30-27-4-2-1-3-25(26)27;;/h1-5,8,11,14,17,20,24H,6-7,9-10,12-13,15-16,19H2,(H,31,33);1H;1H2/t20-,24-;;

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此商品
405607267875554
suitability

Plesiomonas spp., Neisseria spp., bacteria, Aeromonas spp., Pseudomonas spp.

suitability

Plesiomonas spp., Aeromonas spp., Neisseria spp., Pseudomonas spp.

suitability

Enterococcus spp., Streptococcus spp.

suitability

bacteria

Quality Level

200

Quality Level

200

Quality Level

200

Quality Level

100

technique(s)

microbe id | specific enzyme detection: suitable

technique(s)

microbe id | specific enzyme detection: suitable

technique(s)

microbe id | specific enzyme detection: suitable

technique(s)

microbe id | specific enzyme detection: suitable

agency

according to ISO 9308-1:2014

agency

according to ISO 9308-1:2014

agency

according to ISO 7899-2:2000

agency

-

application(s)

agriculture
clinical testing
environmental
food and beverages
pharmaceutical, microbiology

application(s)

agriculture
clinical testing
environmental
food and beverages
pharmaceutical, microbiology

application(s)

environmental
food and beverages
water monitoring, microbiology

application(s)

agriculture
clinical testing
environmental
food and beverages
pharmaceutical, microbiology

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

-

storage temp.

2-8°C

应用

SB-277011-A hydrochloride hydrate has been used:
  • as a dopamine D3 receptor-selective antagonist in rats to test its effect on 4-propyl-9-hydroxynaphthoxazine ([3H]-(+)-PHNO) radiotracer in cerebellum L9/10 and striatum[1]
  • as an acetylcholine inhibitor to test its negative allosteric modulation on Ascaris suum nicotinic acetylcholine receptor (Asu-ACR-16) expressed in Xenopus oocytes and its inhibitory effect on locomotion in Caenorhabditis elegans[2]
  • to test its effect on alcohol consumption in mice[3]

SB-277011-A hydrochloride hydrate may be used in D3 dopamine receptor-mediated cell signaling studies.

生化/生理作用

SB-277011-A is a potent, selective brain-penetrant D3 dopamine receptor antagonist; 80-100x selective for D3 over D2; pKi = 7.95 for hD3 receptor.
SB-277011-A is the most selective D3 dopamine receptor antagonist.
The D3 dopamine receptor antagonist, SB-277011-A inhibits the cocaine-seeking behavior and cocaine-enhances brain stimulation reward in in rats.[4][5] It decreases drug-seeking behavior and may be useful in treatment of cocaine and methamphetamine addiction.[4][5][6]

特点和优势

This compound is featured on the Dopamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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    Zheng-Xiong Xi et al.
    The European journal of neuroscience, 21(12), 3427-3438 (2005-07-20)
    In rats, acute administration of SB-277011A, a highly selective dopamine (DA) D(3) receptor antagonist, blocks cocaine-enhanced brain stimulation reward, cocaine-seeking behaviour and reinstatement of cocaine-seeking behaviour. Here, we investigated whether SB-277011A attenuates cocaine reinforcement as assessed by cocaine self-administration under
    Fudan Zheng et al.
    International journal for parasitology. Drugs and drug resistance, 6(1), 60-73 (2016-04-08)
    Soil-transmitted helminth infections in humans and livestock cause significant debility, reduced productivity and economic losses globally. There are a limited number of effective anthelmintic drugs available for treating helminths infections, and their frequent use has led to the development of
    Krista Spiller et al.
    Psychopharmacology, 196(4), 533-542 (2007-11-07)
    We have previously reported that selective antagonism of brain D3 receptors by SB-277011A or NGB 2904 significantly attenuates cocaine- or nicotine-enhanced brain stimulation reward (BSR). In the present study, we investigated whether the selective D3 receptor antagonists SB-277011A and NGB
    Jeremy G Gilbert et al.
    Synapse (New York, N.Y.), 57(1), 17-28 (2005-04-29)
    Recent studies have shown that the novel dopamine (DA) D3 receptor antagonists SB-277011A and NGB 2904 inhibit cocaine- and/or stress-induced reinstatement of drug-seeking behavior. The present study sought to determine if SB-277011A, NGB 2904, or BP-897 (a mixed D3 agonist/antagonist)
    Amine Bahi et al.
    Alcoholism, clinical and experimental research, 38(9), 2369-2376 (2014-09-27)
    It has been reported that dopamine D3 receptor (D3R) knockout mice display similar ethanol (EtOH) consumption compared to wild types. In addition, studies with D3R pharmacological targeting were inconclusive. In the current study, we used both gain- and loss-of-function approaches

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