SB 242084 dihydrochloride|cas:1049747-87-6|西域试剂

SB 242084 dihydrochloride,98.33%

产品编号：Bellancom-13409A| CAS NO：1049747-87-6| 分子式：C₂₁H₂₁Cl₃N₄O₂| 分子量：467.78

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-13409A	￥1000.00	杭州北京（现货）
Bellancom-13409A	￥1300.00	杭州北京（现货）
Bellancom-13409A	￥6000.00	杭州北京（现货）

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SB 242084 dihydrochloride

产品介绍

SB 242084 dihydrochloride 是一种具有选择性、竞争性和高亲和力的 (pK_i=9.0) 的 5-HT_2C 受体拮抗剂 (可透过血脑屏障)。SB 242084 dihydrochloride 能增加中脑腹侧被盖区 (VTA) 多巴胺能神经元的基础活性和伏隔核中多巴胺的释放。SB 242084 dihydrochloride 还可通过 5-HT_2A 受体增加线粒体基因的表达和氧化代谢。SB 242084 dihydrochloride 在焦虑、抑郁和精神分裂症的阴性症状以及急性器官损伤方面具有较好的研究潜力。

生物活性

SB 242084 dihydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

体外研究

SB 242084 dihydrochloride (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT_2C receptor in SH-SY5Y cells.
SB 242084 dihydrochloride (1-100 nM; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	SH-SY5Y cells
Concentration:	100 nM
Incubation Time:	45 min
Result:	Antagonized 5-HT induced concentration-related increase in PI hydrolysis.

RT-PCR

Cell Line:	RPTC cells
Concentration:	1-100 nM
Incubation Time:	24 h
Result:	Increased FCCP-uncoupled respiration and PGC-1α mRNA expression.

体内研究
(In Vivo)

SB 242084 dihydrochloride (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests.
SB 242084 dihydrochloride (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats.
SB 242084 dihydrochloride (5, 10 mg/kg; i.p.; single) increases the levels of basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens of rats.
SB 242084 dihydrochloride (160-640 µg/kg; i.v.; single) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons, and the bursting activity is also enhanced in the same area, in vivo.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley (CD) rats.
Dosage:	0.1-1 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.

Animal Model:	Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model).
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.

Animal Model:	Rats.
Dosage:	5, 10 mg/kg
Administration:	Intraperitoneal injection; single
Result:	Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley (CD) rats.
Dosage:	0.1-1 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.

Animal Model:	Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model).
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.

Animal Model:	Rats.
Dosage:	5, 10 mg/kg
Administration:	Intraperitoneal injection; single
Result:	Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Sprague-Dawley (CD) rats.
Dosage:	0.1-1 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.

Animal Model:	Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model).
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.

Animal Model:	Rats.
Dosage:	5, 10 mg/kg
Administration:	Intraperitoneal injection; single
Result:	Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 125.5 mg/mL (268.29 mM)

H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1378 mL	10.6888 mL	21.3776 mL
5 mM	0.4276 mL	2.1378 mL	4.2755 mL
10 mM	0.2138 mL	1.0689 mL	2.1378 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (10.69 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (10.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 5 mg/mL (10.69 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (10.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (10.69 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (10.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。