![[D-Lys3]-GHRP-6 (TFA)](/upload/1124/V60045.png)
| 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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| Other Sizes |
| Targets |
[D-Lys3]-GHRP-6 targets the ghrelin receptor (GHS-R1a), where it acts as an antagonist. Ghrelin is a peptide hormone that stimulates growth hormone release and appetite. By blocking the ghrelin receptor, this compound can modulate growth hormone secretion and feeding behavior. It also weakly binds to melanocortin receptors with Ki values of 26-120 μM, suggesting additional interactions with melanocortin signaling pathways involved in energy homeostasis and pigmentation.
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| ln Vitro |
In vitro, [D-Lys3]-GHRP-6 is an antagonist at the ghrelin receptor (GHS-R1a) and weakly binds to melanocortin receptors (Ki = 26-120 μM). The compound's activity is assessed using receptor binding and functional assays. It is used in in vitro studies to investigate ghrelin receptor signaling and its role in feeding behavior, growth hormone secretion, and energy metabolism. Specific IC50 values for receptor binding are not detailed.
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| ln Vivo |
In vivo, [D-Lys3]-GHRP-6 has been studied in rats to observe their memory and learning skills. Different doses of the compound were injected into rats for behavioral studies. These studies suggest that the compound may have effects on cognitive function, likely mediated through ghrelin receptor modulation. However, specific detailed in vivo protocols and efficacy data are limited in the available literature. The compound is for research use only.
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| Enzyme Assay |
The ghrelin receptor (GHS-R1a) binding affinity is assessed using radioligand binding assays. Membrane preparations from cells expressing GHS-R1a are incubated with a radiolabeled ghrelin receptor ligand (e.g., [¹²⁵I]-ghrelin or [³H]-GHRP-6) and various concentrations of [D-Lys3]-GHRP-6. Specific binding is determined, and Ki or IC50 values are calculated from competition binding curves. Functional antagonism is assessed by measuring the compound's ability to inhibit ghrelin-induced intracellular calcium mobilization or cAMP production.
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| Cell Assay |
For cellular studies, cells expressing GHS-R1a (e.g., CHO cells transfected with the receptor) are cultured in appropriate media. Cells are treated with [D-Lys3]-GHRP-6 at various concentrations, and receptor activation is measured using calcium-sensitive fluorescent dyes (e.g., Fluo-4) or by measuring cAMP levels. The compound's ability to inhibit ghrelin-induced signaling is assessed. Cell viability may be assessed using standard assays. The compound is typically dissolved in DMSO or sterile water and diluted in culture media.
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| Animal Protocol |
In vivo studies for [D-Lys3]-GHRP-6 are conducted in rodent models. The compound is administered via intraperitoneal injection or intracerebroventricular injection at various doses. Behavioral assessments for memory and learning include the Morris water maze, novel object recognition, or passive avoidance tests. For feeding behavior studies, food intake is measured. For growth hormone studies, plasma growth hormone levels are measured by ELISA. However, specific detailed protocols are not available.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for [D-Lys3]-GHRP-6 are not reported. As a peptide, the compound is expected to have limited oral bioavailability and short half-life due to rapid proteolytic degradation. The compound has a molecular weight of 930.11 g/mol and a molecular formula of C₄₉H₆₃N₁₃O₆. It is typically stored as a powder at -20°C and protected from light. For in vivo administration, the peptide is typically dissolved in saline or sterile water.
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| Toxicity/Toxicokinetics |
Toxicological data for [D-Lys3]-GHRP-6 are limited. As a research peptide, comprehensive toxicology studies have not been reported. The compound should be handled with appropriate safety precautions in laboratory settings. As a ghrelin receptor antagonist, potential effects on feeding behavior, growth hormone secretion, and metabolism should be considered. The compound is for research use only and not for human consumption.
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| Additional Infomation |
[D-Lys3]-GHRP-6 is a synthetic hexapeptide ghrelin receptor (GHS-R1a) antagonist with weak binding to melanocortin receptors (Ki = 26-120 μM). It is used in neuropharmacological research on memory, learning, feeding behavior, and growth hormone regulation. No clinical trials or approvals exist. For research use only.
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| Molecular Formula |
C49H63N13O6
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| Molecular Weight |
930.10800
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| Exact Mass |
929.502
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| CAS # |
136054-22-3
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| PubChem CID |
5311279
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
5.893
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
27
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| Heavy Atom Count |
68
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| Complexity |
1640
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| Defined Atom Stereocenter Count |
6
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| SMILES |
NCCCC[C@@H](C(N)=O)NC([C@H](NC([C@@H](NC([C@H](NC([C@H](NC([C@@H](N)CC1=CN=CN1)=O)CC2=CNC3=CC=CC=C23)=O)CCCCN)=O)CC4=CNC5=CC=CC=C45)=O)CC6=CC=CC=C6)=O
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| InChi Key |
MGSNWNLPMHXGDD-DFWOJPNQSA-N
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| InChi Code |
InChI=1S/C49H63N13O6/c50-20-10-8-18-39(44(53)63)58-47(66)41(22-30-12-2-1-3-13-30)61-49(68)43(24-32-27-56-38-17-7-5-15-35(32)38)62-46(65)40(19-9-11-21-51)59-48(67)42(23-31-26-55-37-16-6-4-14-34(31)37)60-45(64)36(52)25-33-28-54-29-57-33/h1-7,12-17,26-29,36,39-43,55-56H,8-11,18-25,50-52H2,(H2,53,63)(H,54,57)(H,58,66)(H,59,67)(H,60,64)(H,61,68)(H,62,65)/t36-,39-,40+,41+,42+,43-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[(2R)-2-[[(2S)-2-[[(2R)-6-amino-2-[[(2R)-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]amino]hexanamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0751 mL | 5.3757 mL | 10.7514 mL | |
| 5 mM | 0.2150 mL | 1.0751 mL | 2.1503 mL | |
| 10 mM | 0.1075 mL | 0.5376 mL | 1.0751 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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