名称 | Capromorelin Tartrate |
描述 | Capromorelin Tartrate (CP 424391-18) is a potent, orally active growth hormone secretagogue receptor (GHSR) agonist (Ki: 7 nM for hGHS-R1a). |
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]. |
体外活性 | Capromorelin在大鼠脑垂体细胞培养中促进GH释放(EC50:3 nM)[1]。 |
体内活性 | Capromorelin在啮齿动物模型中展现出了增强的肠道吸收能力,并且在药代动力学属性上表现出众,包括在两种动物模型中的高生物利用度(F(rat)=65%,F(dog)=44%)。Capromorelin能够在麻醉状态的大鼠模型中刺激GH释放(ED50: 0.05 mg/kg iv)。接受capromorelin(30 mg/mL)治疗的狗,其食物消耗量显著高于接受安慰剂治疗的狗。所有接受capromorelin治疗的狗体重增加了0.52 kg,这一增加量高于安慰剂组。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 100 mg/mL (152.51 mM)
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关键字 | Inhibitor | Growth hormone secretagogue receptor | GHSR | Capromorelin | inhibit | Capromorelin Tartrate |
相关产品 | TM-N1324 | Obestatin (rat) acetate | NF-56-EJ40 hydrochloride | Anamorelin | CJC-1295 acetate(863288-34-0 free base) | Ibutamoren Mesylate | hGPR91 antagonist 1 | YIL 781 | AnaMorelin hydrochloride | Relamorelin | L-692429 | Cortistatin-8 acetate |
相关库 | 经典已知活性库 | 已知活性化合物库 | NO PAINS 化合物库 | GPCR靶点分子库 | 临床期小分子药物库 | 膜蛋白靶向化合物库 | 口服活性化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库 |