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Capromorelin Tartrate

Capromorelin Tartrate

产品编号 TQ0022   CAS 193273-69-7
别名: 卡普瑞林酒石酸盐, CP 424391-18

Capromorelin Tartrate (CP 424391-18) 是口服有活性的 growth hormone secretagogue receptor 有效激动剂,能够作用于 hGHS-R1a(Ki:7 nM)。

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Capromorelin Tartrate Chemical Structure
Capromorelin Tartrate, CAS 193273-69-7
规格 价格/CNY 货期 数量
1 mg ¥ 263 现货
2 mg ¥ 371 现货
5 mg ¥ 531 现货
10 mg ¥ 931 现货
25 mg ¥ 1,990 现货
50 mg ¥ 3,680 现货
100 mg ¥ 5,280 现货
1 mL * 10 mM (in DMSO) ¥ 838 现货
其他形式的 Capromorelin Tartrate:
产品目录号及名称: Capromorelin Tartrate (TQ0022)
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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 Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a).
靶点活性 hGHS-R1a:7 nM (Ki)
体外活性 Capromorelin stimulates GH release in rat pituitary cell cultures (EC50: 3 nM) [1].
体内活性 Capromorelin shows enhanced intestinal absorption in rodent models and exhibits superior pharmacokinetic properties, including high bioavailabilities in two animal species [F(rat)=65%, F(dog)=44%][1]. Capromorelin stimulates GH release in the anesthesized rat model (ED50: 0.05 mg/kg iv) [1]. Dogs receiving capromorelin (30 mg/mL) have food consumption that is significantly greater than dogs treated with placebo. All dogs in the capromorelin group gain weight by 0.52 kg, more than that of the placebo group [2].
激酶实验 Membranes are prepared from HEK293 cells stably transfected with the human GHS-R1a receptor cDNA in the plasmid pcDNA3.1neo. Competition radioligand binding assays are performed in 96-well format with GF/C filters pre-soaked in 0.3% polyethyleneimine. Assays are performed at room temperature for 1 h in duplicate using 50 pM [125I]-ghrelin and 1 μg membrane per well in 50 mM HEPES, pH 7.4, 10 mM MgCl2, 0.2% bovine serum albumin and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/mL leupeptin. The membranes are harvested and washed three times with ice-cold ish buffer containing 50 mM HEPES, pH 7.4 and 10 mM MgCl2. IC50 and Ki values are determined using Prism. The Kd of [125I]-ghrelin at membranes expressing human GHS receptors is calculated to be 0.2 nM [1].
动物实验 The study tested capromorelin flavored oral solution with 30 mg/mL of capromorelin compared to a matched placebo flavored oral solution treatment (which contains all the ingredients of the formulation without capromorelin) administered for 4 days. Dogs are randomized into two groups, with Group 1 receiving placebo (0.1 mL/kg) and Group 2 receiving 3.0 mg/kg. Both groups are treated once a day at approximately 9 AM each day. The first day of dosing is considered Day 0. The placebo and test drug are administered by a syringe placed in the corner of the mouth. The Day 0 weight is used for dose calculations [2].
别名 卡普瑞林酒石酸盐, CP 424391-18
分子量 655.7
分子式 C32H41N5O10
CAS No. 193273-69-7

存储

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

溶解度

DMSO: 100 mg/mL (152.51 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 1 mM 1.5251 mL 7.6254 mL 15.2509 mL 38.1272 mL
5 mM 0.305 mL 1.5251 mL 3.0502 mL 7.6254 mL
10 mM 0.1525 mL 0.7625 mL 1.5251 mL 3.8127 mL
20 mM 0.0763 mL 0.3813 mL 0.7625 mL 1.9064 mL
50 mM 0.0305 mL 0.1525 mL 0.305 mL 0.7625 mL
100 mM 0.0153 mL 0.0763 mL 0.1525 mL 0.3813 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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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. 2. Zollers B, et al. Capromorelin oral solution (ENTYCE?) increases food consumption and body weight when administered for 4 consecutive days to healthy adult Beagle dogs in a randomized, masked, placebo controlled study. BMC Vet Res. 2017 Jan 5;13(1):10.
TM-N1324 hGPR91 antagonist 1 Relamorelin CJC-1295 acetate(863288-34-0 free base) PF-5190457 Obestatin (rat) acetate Anamorelin TC-G-1008

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌药物库 口服活性化合物库 已知活性化合物库 经典已知活性库 临床期小分子药物库 药物功能重定位化合物库 NO PAINS 化合物库 GPCR靶点分子库

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
g
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
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% ddH2O
计算 重置

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

Capromorelin Tartrate 193273-69-7 GPCR/G Protein GHSR Inhibitor Growth hormone secretagogue receptor Capromorelin 卡普瑞林酒石酸盐 inhibit CP 424391-18 inhibitor

 

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