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BRL-15572 dihydrochloride

产品编号 T6423 CAS 193611-72-2

别名: 四氢罂粟碱盐酸盐, BRL 15573 dihydrochloride

BRL-15572 dihydrochloride (BRL 15573 dihydrochloride) 是一种 5-HT1D 受体拮抗剂，pKi 为 7.9，对 5-HT1A 和 5-HT2B 受体也显示出相当大的亲和力，其选择性是 5-HT1B 受体的 60 倍。

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BRL-15572 dihydrochloride Chemical Structure

BRL-15572 dihydrochloride, CAS 193611-72-2

规格	价格/CNY	货期
1 mg	￥ 193	现货
5 mg	￥ 417	现货
10 mg	￥ 587	现货
25 mg	￥ 984	现货
50 mg	￥ 1,770	现货
100 mg	￥ 2,496	现货
1 mL * 10 mM (in DMSO)	￥ 441	现货

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其他形式的 BRL-15572 dihydrochloride:

BRL-15572 hydrochloride
询价
BRL 15572
询价

选择批次

纯度: 99.8%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	BRL-15572 dihydrochloride (BRL 15573 dihydrochloride) is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.
靶点活性	5-HT1A:7.7(pKi), 5-HT2B:7.4(pKi), 5-HT2A:6.6(pKi), 5-HT1D:7.9(pKi), 5-HT7:6.3(pKi)
体外活性	BRL-15572 displays high affinity and selectivity for h5-HT1D receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 μM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors. [1] In human atrial appendages, the electrically evoked tritium overflow is inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors). [2] The inhibitory effect of 5-HT on the K+-evoked overflow of glutamate is antagonized by the h5-HT1D receptor ligand BRL-15572. BRL-15572 (1 μM) is unable to modify the effect of 5-HT at the autoreceptor regulating [3H]5-HT release. [3] The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247. [4]
体内活性	In diabetic pithed rats, administration of the selective 5-HT1D receptor antagonist BRL-15572 (2 mg/kg) does not modify the decreased HR induced by vagal electrical stimulation. The effects of L-694,247 (50 μg/kg), a selective agonist for non-rodent 5-HT1B and 5-HT1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572. [5]
细胞实验	[35S]GTPγS binding studies. [35S]GTPγS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1 × 106 cells are preincubated at 30°C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 μ M), with or without BRL-15572. The reaction is started by the addition of 10 μL of [35S]GTPγS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30°C. Non-specific binding is determined by addition of unlabelled GTPγS (10 μM), prior to the addition of cells. The reaction is stopped by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Radioactivity is determined by liquid scintillation spectrometry.(Only for Reference)

别名	四氢罂粟碱盐酸盐, BRL 15573 dihydrochloride
分子量	479.87
分子式	C25H27ClN2O·2HCl
CAS No.	193611-72-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 89 mg/mL (185.5 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 38 mg/mL (79.2 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	2.0839 mL	10.4195 mL	20.839 mL	52.0974 mL
	5 mM	0.4168 mL	2.0839 mL	4.1678 mL	10.4195 mL
	10 mM	0.2084 mL	1.0419 mL	2.0839 mL	5.2097 mL
	20 mM	0.1042 mL	0.521 mL	1.0419 mL	2.6049 mL
	50 mM	0.0417 mL	0.2084 mL	0.4168 mL	1.0419 mL
DMSO	100 mM	0.0208 mL	0.1042 mL	0.2084 mL	0.521 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Price GW, et al. Naunyn Schmiedebergs Arch Pharmacol. 1997, 356(3), 312-320. 2. Schlicker E, et al. Naunyn Schmiedebergs Arch Pharmacol. 1997, 356(3), 321-327. 3. Marcoli M, et al. Br J Pharmacol. 1999, 126(3), 607-612. 4. Calama E, et al. Clin Exp Pharmacol Physiol. 2005, 32(10), 894-900. 5. García M, et al. Clin Exp Pharmacol Physiol. 2007 Nov;34(11):1199-206.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

BRL-15572 dihydrochloride 193611-72-2 GPCR/G Protein Neuroscience 5-HT Receptor h5-HT1D BRL 15572 dihydrochloride BRL-15573 BRL15573 Dihydrochloride BRL-15572 四氢罂粟碱盐酸盐 BRL 15572 Dihydrochloride BRL 15573 BRL 15572 BRL15572 BRL 15573 dihydrochloride BRL-15573 Dihydrochloride BRL15573 Inhibitor Serotonin Receptor BRL15572 dihydrochloride 5-hydroxytryptamine Receptor inhibit BRL 15573 Dihydrochloride BRL15572 Dihydrochloride BRL-15572 Dihydrochloride inhibitor

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BRL-15572 dihydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords