Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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)。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (152.51 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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