1. GPCR/G Protein
  2. GHSR
  3. Capromorelin Tartrate

Capromorelin Tartrate (Synonyms: CP 424391-18)

Cat. No.: HY-15243 Purity: 98.19%
Handling Instructions

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

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

Capromorelin Tartrate Chemical Structure

Capromorelin Tartrate Chemical Structure

CAS No. : 193273-69-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
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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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with Ki 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].

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].

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

SMILES

O=C([[email protected]@H]([[email protected]@H](O)C(O)=O)O)O.CC(C)(N)C(N[[email protected]](COCC1=CC=CC=C1)C(N(C[[email protected]]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: 

DMSO : ≥ 100 mg/mL (152.51 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (3.81 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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 Ki values are determined using Prism by GraphpadTM. The Kd 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

Purity: 98.19%

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Keywords:

CapromorelinCP 424391-18GHSRGrowth hormone secretagogue receptorInhibitorinhibitorinhibit

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Product Name:
Capromorelin Tartrate
Cat. No.:
HY-15243
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