Capromorelin-Tartrate-CP-424391-18-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECapromorelin TartrateCat. No.: HY-15243CAS No.: 193273-69-7Synonyms: CP 424391-18分式: CHNO分量: 655.7作靶點(diǎn): GHSR作通路: GPCR/G Protein儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (152.

2、51 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.5251 mL 7.6254 mL 15.2509 mL5 mM 0.3050 mL 1.5251 mL 3.0502 mL10 mM 0.1525 mL 0.7625 mL 1.5251 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性

3、，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.81 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.81 mM); Clear solution1/3 Master of Small Molecules 您邊的抑

4、制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.81 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Capromorelin Tartrate種可服的，有效的growth hormone secretagogue receptor (GHSR)激動(dòng)劑，對(duì)hGHS-R1a的Ki值為 7 nM。IC50 & Target Ki: 7 nM (hGHS-R1a) 2體外研究 Capromorelin stimulates GH release in rat pi

5、tuitary cell cultures with EC50 of 3 nM 2.體內(nèi)研究 Dogs receiving capromorelin (30 mg/mL) have food consumption that is significantly greater than dogstreated with placebo. All dogs in the capromorelin group gain weight by 0.52 kg, more than that of placebogroup 1. Capromorelin shows enhanced intestinal

6、 absorption in rodent models and exhibits superiorpharmacokinetic properties, including high bioavailabilities in two animal species F(rat)=65%, F(dog)=44%2. Capromorelin stimulates GH release in anesthesized rat model, with ED50 of 0.05 mg/kg iv 2.PROTOCOLKinase Assay 2 Membranes are prepared from

7、HEK293 cells (ATCC) stably transfected with the human GHS-R1a receptorcDNA in the plasmid pcDNA3.1neo. Competition radioligand binding assays are performed in 96-well formatwith GF/C filters pre-soaked in 0.3% polyethyleneimine. Assays are performed at room temperature for 1 h induplicate using 50 p

8、M 125I-ghrelin and 1 g membrane per well in 50 mM HEPES, pH 7.4, 10 mM MgCl2,0.2% bovine serum albumin and the following protease inhibitors: 100 g/mL bacitracin, 100 g/mLbenzamidine, 5 g/mL aprotinin, 5 g/mL leupeptin. The membranes are harvested and washed three timeswith ice-cold ish buffer conta

9、ining 50 mM HEPES, pH 7.4 and 10 mM MgCl2. IC50 and Ki values aredetermined using Prism by GraphpadTM. The Kd of 125I-ghrelin at membranes expressing human GHSreceptors is calculated to be 0.2 nM.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Th

10、e study tested capromorelin flavored oral solution with 30 mg/mL of capromorelin compared to a matchedAdministration 1 placebo flavored oral solution treatment (which contains all the ingredients of the formulation withoutcapromorelin) administered for 4 days. Dogs are randomized into two groups, wi

11、th 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 AMeach day. The first day of dosing is considered Day 0. The placebo and test drug are administered by asyringe placed in the corner of the mouth. The Day 0 weight is used f

12、or dose calculations.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zollers B, et al. Capromorelin oral solution (ENTYCE) increases food consumption and body weight when administered for 42/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEconsecutive days to healthy adult Beagle dogs in a randomized, masked, placebo controlled study. BMC Vet Res. 2017 Jan 5;13(1):10.2. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg MedChem. 2003 Feb 20;11(4):581-90.McePdfH