| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Capromorelin, formerly known as CP-424,391, is a growth hormone secretagogue and ghrelin mimetic ( hGHS-R1a K(i)=7 nM, rat pituicyte EC(50)=3 nM). Preliminary research has demonstrated that the medication directly increases growth hormone and insulin growth factor 1 (IGF-1). Capromorelin demonstrated improved pharmacokinetic characteristics, such as high bioavailabilities in two animal species [F(rat)=65%, F(dog)=44%], and improved intestinal absorption in rodent models. In canine models, this short-duration GHS was orally bioavailable, and it was chosen as a development candidate for the management of musculoskeletal frailty in the elderly.
| Targets |
hGHS-R1a ( Ki = 7 nM )
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|---|---|
| ln Vitro |
Capromorelin induces the release of growth hormone in rat pituitary cell cultures with EC50 of 3 nM[2].
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| ln Vivo |
The food consumption of dogs treated with capromorelin (30 mg/mL) is significantly higher than that of dogs treated with a placebo. More than the placebo group, all dogs in the capromorelin group gained weight by 0.52 kg[1]. In rodent models, capromolelin demonstrates improved intestinal absorption and superior pharmacoKinetic characteristics, such as high bioavailabilities in two animal species [F(dog)=44%, F(rat)=65%]. Reference [2]. With an ED50 of 0.05 mg/kg iv, capromolelin stimulates the release of growth hormone in a model of anesthetized rats[2].
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| Enzyme Assay |
The human GHS-R1a receptor cDNA in the plasmid pcDNA3.1neo is transfected into HEK293 cells (ATCC) to produce membranes. Competition radioligand binding assays are run in 96-well format using GF/C filters that have been pre-soaked in 0.3% polyethyleneimine. Tests are run in duplicate at room temperature for one hour, employing 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 subsequent protease inhibitors: 100 μg/mL benzamidine, 100 μg/mL bacitracin, 5 μg/mL aprotinin, and 5 μg/mL leupeptin. After harvesting the membranes, they are rinsed three times in an ice-cold buffer that has pH 7.4, 50 mM HEPES, and 10 mM MgCl2. Prism by GraphpadTM is used to calculate the IC50 and Ki values. It is determined that the Kd of [125I]-ghrelin at membranes expressing human GHS receptors is 0.2 nM.
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| Animal Protocol |
The study evaluated a flavored oral solution containing 30 mg/mL of capromorelin in comparison to a matched placebo-flavored oral solution treatment that was given for four days and contained all the formulation's ingredients but no capromorelin. Two groups of dogs are randomly assigned; Group 1 receives a placebo (0.1 mL/kg), while Group 2 receives 3.0 mg/kg. Each day, at around nine in the morning, both groups receive the same treatment. Day 0 is the first day of medication. A syringe inserted into the mouth's corner is used to administer both the test medication and the placebo. When calculating doses, the Day 0 weight is utilized.
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| References |
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| Molecular Formula |
C32H41N5O10
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|---|---|
| Molecular Weight |
655.705
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| Exact Mass |
655.29
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| Elemental Analysis |
C, 58.62; H, 6.30; N, 10.68; O, 24.40
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| CAS # |
193273-69-7
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| Related CAS # |
193273-66-4; 193273-69-7 (tartrate)
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| Appearance |
Solid powder
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| SMILES |
CC(C)(C(=O)N[C@H](COCC1=CC=CC=C1)C(=O)N2CCC3=NN(C(=O)[C@@]3(C2)CC4=CC=CC=C4)C)N.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
MJGRJCMGMFLOET-MYPSAZMDSA-N
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| InChi Code |
InChI=1S/C28H35N5O4.C4H6O6/c1-27(2,29)25(35)30-22(18-37-17-21-12-8-5-9-13-21)24(34)33-15-14-23-28(19-33,26(36)32(3)31-23)16-20-10-6-4-7-11-20;5-1(3(7)8)2(6)4(9)10/h4-13,22H,14-19,29H2,1-3H3,(H,30,35);1-2,5-6H,(H,7,8)(H,9,10)/t22-,28-;1-,2-/m11/s1
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| Chemical Name |
N-[(2R)-1-[(3aR)-3a-benzyl-2-methyl-3-oxo-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]-1-oxo-3-phenylmethoxypropan-2-yl]-2-amino-2-methylpropanamide;(2R,3R)-2,3-dihydroxybutanedioic acid
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| Synonyms |
Capromorelin tartrate; CP424,391; CP-424391; CP-424,391; CP 424,391;CP 424391; CP424391; CP-424,391-18
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~152.5 mM)
H2O: ~100 mg/mL (~152.5 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (76.25 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5251 mL | 7.6253 mL | 15.2506 mL | |
| 5 mM | 0.3050 mL | 1.5251 mL | 3.0501 mL | |
| 10 mM | 0.1525 mL | 0.7625 mL | 1.5251 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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