货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S87300-5mg买3赠1	≥97%	￥3250.00 S87300-5mg ￥3250.00 现货（买3赠1）	5 5	-	-	-	-
S87300-10mg买3赠1	≥97%	￥4650.00 S87300-10mg ￥4650.00 现货（买3赠1）	7 7	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S87300-5mg买3赠1

≥97%

￥3250.00

S87300-10mg买3赠1

≥97%

￥4650.00

产品描述：

Camicinal (GSK962040) is a small molecule, selective motilin receptor agonist with pEC50 of 7.9.

靶点：

pEC50: 7.9 (Motilin Receptor)

体外研究：

Camicinal (GSK962040) had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes. In rabbit gastric antrum, Camicinal (GSK962040) 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 (GSK962040) were, respectively, 10.4 ± 0.01 (n = 770), 7.3 ± 0.29 (n = 4) and 7.9 ± 0.09 (n = 17). Camicinal (GSK962040) activated the dog motilin receptor (pEC50 5.79; intrinsic activity 0.72, compared with [Nle13]-motilin) [2]. Camicinal (GSK962040) was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM

体内研究：

Camicinal (GSK962040) (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 < 0.05). Camicinal (GSK962040) induced phasic contractions, the duration of which was dose-related (48 and 173 min for 3 and 6 mg kg 1), driven by mean plasma concentrations >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 (GSK962040) 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). Camicinal (GSK962040) strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.355 ml	11.777 ml	23.554 ml
5 mM	0.471 ml	2.355 ml	4.711 ml
10 mM	0.236 ml	1.178 ml	2.355 ml
50 mM	0.047 ml	0.236 ml	0.471 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置