Spiperone hydrochloride Spiroperidol hydrochloride|cas:2022-29-9|西域试剂

Spiperone hydrochloride Spiroperidol hydrochloride,99.0%

产品编号：Bellancom-B1371A| CAS NO：2022-29-9| 分子式：C₂₃H₂₇ClFN₃O₂| 分子量：431.93

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-B1371A		￥800.00	杭州北京（现货）

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Spiperone hydrochloride Spiroperidol hydrochloride

产品介绍

Spiperone hydrochloride (Spiroperidol hydrochloride) 是一种选择性的多巴胺 D₂ 受体 (D₂，D₃，D₄，D₁ 和 D₅ 受体的 K_i 值分别为 0.06 nM，0.6 nM，0.08 nM，~350 nM，~3500 nM) 和 5-HT_2A/5-HT_1A 受体 (K_i 为1 nM/49 nM) 拮抗剂。Spiperone hydrochloride 也是一种选择性的 α1B-肾上腺素受体 (α1B-adrenoceptor) 拮抗剂。Spiperone hydrochloride 激活钙激活的氯离子通道 (CaCC)。抗精神病和抗炎作用。

生物活性

Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D₂ receptor (K_i values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors, respectively) and 5-HT_2A/5-HT_1A receptor (K_is of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities^[4]^[5].

体外研究

Spiperone is a potent intracellular Ca²⁺ enhancer (EC₅₀=9.3 μM) and stimulates intracellular Ca²⁺ through a protein tyrosine kinase-coupled phospholipase C-dependent pathway, which results in increased secretion of Cl^- in Calu-3 and CFBE41o^- cell monolayers.
Spiperone significantly decreases the production of nitric oxide in lipopolysaccharide-stimulated BV-2 microglia cells, primary microglia and primary astrocyte cultures. Spiperone also significantly inhibits nitric oxide production in ATP-stimulated primary microglia cultures. Spiperone markedly decreases the production of TNF-α in BV-2 microglia cells. Spiperone attenuates the expression of inducible nitric oxide synthase and proinflammatory cytokines such as IL-1β and TNF-α at mRNA levels in BV-2 microglia cells.

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

体内研究

Spiperone (1.5 mg/kg; intraperitoneal injection; on days 1, 3, 6, 7, and 13-21; C57Bl/6 mice) treatment reduces infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevents the growth of the connective tissue in the parenchyma of Bleomycin lungs^[6].

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

Animal Model:	C57Bl/6 mice (7-8-week-old) induced pulmonary fibrosis by Bleomycin^[6]
Dosage:	1.5 mg/kg
Administration:	Intraperitoneal injection; on days 1, 3, 6, 7, and 13-21
Result:	Reduced infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevented the growth of the connective tissue in the parenchyma of bleomycin lungs.

体内研究

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

Animal Model:	C57Bl/6 mice (7-8-week-old) induced pulmonary fibrosis by Bleomycin^[6]
Dosage:	1.5 mg/kg
Administration:	Intraperitoneal injection; on days 1, 3, 6, 7, and 13-21
Result:	Reduced infiltration of the alveolar interstitium and alveolar ducts with inflammatory cells and prevented the growth of the connective tissue in the parenchyma of bleomycin lungs.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (289.40 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3152 mL	11.5759 mL	23.1519 mL
5 mM	0.4630 mL	2.3152 mL	4.6304 mL
10 mM	0.2315 mL	1.1576 mL	2.3152 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.82 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。