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Camicinal

产品编号 T11508 CAS 923565-21-3

别名: GSK962040

Camicinal is a selective motilin receptor agonist (pEC50: 7.9). 在相同实验条件下，摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性，但盐形式 Camicinal hydrochloride 的水溶性和稳定性通常比游离态更好。

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Camicinal, CAS 923565-21-3

规格	价格/CNY	货期
2 mg	￥ 1,730	5日内发货
5 mg	￥ 2,680	5日内发货
25 mg	￥ 8,930	6-8周
50 mg	￥ 11,600	6-8周
100 mg	￥ 16,200	6-8周
1 mL * 10 mM (in DMSO)	￥ 2,520	5日内发货

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Camicinal 的其他形式现货产品:

Camicinal hydrochloride

其他形式的 Camicinal:

Camicinal hydrochloride
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Camicinal is a selective motilin receptor agonist (pEC50: 7.9).
靶点活性	Motilin receptor:(pEC50)7.9
体外活性	Camicinal ?had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal ?300 nmol L 1-10 μmol L 1 caused a prolonged facilitation of the amplitude of cholinergically mediated contractions, to a maximum of 248 ± 47% at 3 μmol L 1. The pEC50 values for motilin, erythromycin and Camicinal ?were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17) . Camicinal ?activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) . Camicinal ?was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM .
体内活性	Camicinal (5 mg free base kg 1) also produced an increase in total faecal weight over the 2-h postdose period (21.2 ± 4.5 g;?P 1.14 μmol L 1.?After the effects of GSK962040 faded, migrating motor complex (MMC) activity returned.?Migrating motor complex restoration was unaffected by 3 mg kg 1 GSK962040 but at 6 mg kg 1, MMCs returned 253 min after dosing, compared with 101 min after saline (n = 5 each) .?he oral bioavailability (Fpo) of Camicinal (GSK962040) was found to be 48 ( 13%.?Camicinal ?shows a long lasting effect (T1/2 ) 46.9 ( 5.0 min at 3 μM) when compared with the short-lived effect of [Nle13]motilin (T1/2 ) 11.4 ( 1.5 min at 0.3 μM) [3].?Camicinal ?strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only .

别名	GSK962040
分子量	424.55
分子式	C25H33FN4O
CAS No.	923565-21-3

存储

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

溶解度

DMSO: 100 mg/mL (235.54 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3554 mL	11.7772 mL	23.5544 mL	58.8859 mL
	5 mM	0.4711 mL	2.3554 mL	4.7109 mL	11.7772 mL
	10 mM	0.2355 mL	1.1777 mL	2.3554 mL	5.8886 mL
	20 mM	0.1178 mL	0.5889 mL	1.1777 mL	2.9443 mL
	50 mM	0.0471 mL	0.2355 mL	0.4711 mL	1.1777 mL
	100 mM	0.0236 mL	0.1178 mL	0.2355 mL	0.5889 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

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参考文献

1. Sanger, G.J., et al., GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. Neurogastroenterol Motil, 2009. 21(6): p. 657-64, e30-1. 2. Leming, S., et al., GSK962040: a small molecule motilin receptor agonist which increases gastrointestinal motility in conscious dogs. Neurogastroenterol Motil, 2011. 23(10): p. 958-e410. 3. Westaway, S.M., et al., Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-pi peridinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. J Med Chem, 2009. 52(4): p. 1180-9. 4. Broad, J., et al., Regional- and agonist-dependent facilitation of human neurogastrointestinal functions by motilin receptor agonists. Br J Pharmacol, 2012. 167(4): p. 763-74.

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

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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。

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