Capromorelin Tartrate (Synonyms: CP 424391-18)

Name: Capromorelin Tartrate
Brand: MedChemExpress
SKU: HY-15243
Rating: 4.5 (1 reviews)

Cat. No.: HY-15243 Purity: 98.71%: FAQs
Data Sheet SDS COA Handling Instructions

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Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with K_i of 7 nM for hGHS-R1a.

For research use only. We do not sell to patients.

Capromorelin Tartrate Chemical Structure

CAS No. : 193273-69-7

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 101	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 101	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 260	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 460	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 1 publication(s) in Google Scholar

Other Forms of Capromorelin Tartrate:

Capromorelin Get quote

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Biological Activity
Protocol
Purity & Documentation
References
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Description

Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with K_i of 7 nM for hGHS-R1a.

IC₅₀ & Target

Ki: 7 nM (hGHS-R1a)^[2]

In Vitro

Capromorelin stimulates GH release in rat pituitary cell cultures with EC₅₀ of 3 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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 placebo group^[1]. 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%]^[2]. Capromorelin stimulates GH release in anesthesized rat model, with ED₅₀ of 0.05 mg/kg iv^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

655.70

Formula

C₃₂H₄₁N₅O₁₀

CAS No.

193273-69-7

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]([C@@H](O)C(O)=O)O)O.CC(C)(N)C(N[C@H](COCC1=CC=CC=C1)C(N(C[C@]23CC4=CC=CC=C4)CCC2=NN(C)C3=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (152.51 mM; Need ultrasonic)

DMSO : 100 mg/mL (152.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5251 mL	7.6254 mL	15.2509 mL
5 mM	0.3050 mL	1.5251 mL	3.0502 mL
10 mM	0.1525 mL	0.7625 mL	1.5251 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (76.25 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.71%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (259 KB) HNMR (286 KB) LCMS (98 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. [Content Brief]

Kinase Assay ^[2]	Membranes are prepared from HEK293 cells (ATCC) 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 K_i values are determined using Prism by Graphpad^TM. The K_d of [¹²⁵I]-ghrelin at membranes expressing human GHS receptors is calculated to be 0.2 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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. [Content Brief] [2]. Carpino PA, et al. Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.5251 mL	7.6254 mL	15.2509 mL	38.1272 mL
	5 mM	0.3050 mL	1.5251 mL	3.0502 mL	7.6254 mL
	10 mM	0.1525 mL	0.7625 mL	1.5251 mL	3.8127 mL
	15 mM	0.1017 mL	0.5084 mL	1.0167 mL	2.5418 mL
	20 mM	0.0763 mL	0.3813 mL	0.7625 mL	1.9064 mL
	25 mM	0.0610 mL	0.3050 mL	0.6100 mL	1.5251 mL
	30 mM	0.0508 mL	0.2542 mL	0.5084 mL	1.2709 mL
	40 mM	0.0381 mL	0.1906 mL	0.3813 mL	0.9532 mL
	50 mM	0.0305 mL	0.1525 mL	0.3050 mL	0.7625 mL
	60 mM	0.0254 mL	0.1271 mL	0.2542 mL	0.6355 mL
	80 mM	0.0191 mL	0.0953 mL	0.1906 mL	0.4766 mL
	100 mM	0.0153 mL	0.0763 mL	0.1525 mL	0.3813 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Capromorelin Tartrate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Capromorelin193273-69-7CP 424391-18GHSRGrowth hormone secretagogue receptorGhrelin receptorInhibitorinhibitorinhibit

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Capromorelin Tartrate (Synonyms: CP 424391-18)

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Complete Stock Solution Preparation Table

Capromorelin Tartrate Related Classifications

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