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| Other Sizes |
| Targets |
des-Gln14-Ghrelin specifically targets the ghrelin receptor (GHS-R1a), a G protein-coupled receptor that is the primary mediator of ghrelin's effects on growth hormone release, appetite, and metabolism. It acts as an endogenous agonist, binding to and activating this receptor to induce similar effects to ghrelin. Its production via alternative splicing highlights the complexity of the ghrelinergic system.
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| ln Vitro |
In vitro, des-Gln14-Ghrelin is a potent activator of the ghrelin receptor. It potently induces the upregulation of intracellular calcium ([Ca2+]i) in CHO cells expressing the ghrelin receptor (CHO-GHSR62 cells) with an EC50 of 2.4 nM. This potent activity confirms its role as a key endogenous agonist for the GHS-R1a.
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| ln Vivo |
In vivo, des-Gln14-Ghrelin stimulates the release of growth hormone (GH). This activity mirrors the primary function of ghrelin and confirms that this alternatively spliced product is a bioactive peptide capable of activating the GHS-R1a axis to promote GH secretion. This makes it a useful tool for studying GH regulation.
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| Enzyme Assay |
For non-cellular in vitro receptor binding assays, des-Gln14-Ghrelin is characterized using radioligand binding techniques with membrane preparations from cells expressing the ghrelin receptor. These assays determine its binding affinity and confirm its specificity for the GHS-R1a. Its identification as a second endogenous ligand was confirmed through such studies.
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| Cell Assay |
For in vitro cellular assays, the activity of des-Gln14-Ghrelin is evaluated in cells expressing the ghrelin receptor, such as CHO-GHSR62 cells. A key functional assay measures the agonist-induced mobilization of intracellular calcium. Cells are loaded with a calcium-sensitive fluorescent dye, and the increase in fluorescence upon peptide addition is measured to determine its EC50, which is 2.4 nM.
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| Animal Protocol |
In vivo animal studies with des-Gln14-Ghrelin are typically conducted in rodent models to study its effects on growth hormone release and metabolism. The peptide is administered via injection, and blood samples are collected to measure GH levels. These studies confirm its activity as a GH secretagogue and are used to investigate the physiological role of this alternative ghrelin ligand.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for des-Gln14-Ghrelin are not extensively documented. As a peptide, its oral bioavailability is likely low, and it would require parenteral administration for in vivo studies. Its half-life in the circulation is expected to be short due to rapid degradation by peptidases. For research purposes, it is typically administered via injection to ensure it reaches its target receptors.
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| Toxicity/Toxicokinetics |
Toxicological data for des-Gln14-Ghrelin are not applicable. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
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| References | |
| Additional Infomation |
des-Gln14-Ghrelin is an endogenous peptide and the second ligand for the ghrelin receptor (GHS-R1a), produced by alternative splicing. It potently induces Ca2+ release in cells expressing the receptor with an EC50 of 2.4 nM and stimulates GH release in vivo. It is a valuable research tool for studying the ghrelin system.
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| Molecular Formula |
C142H237N43O40
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|---|---|
| Molecular Weight |
3186.66531157494
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| Exact Mass |
3185.786
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| CAS # |
293735-04-3
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| PubChem CID |
137699510
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| Appearance |
White to off-white solid powder
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| LogP |
-17.3
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| Hydrogen Bond Donor Count |
44
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| Hydrogen Bond Acceptor Count |
49
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| Rotatable Bond Count |
114
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| Heavy Atom Count |
225
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| Complexity |
7240
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| Defined Atom Stereocenter Count |
26
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| SMILES |
C(N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(N1CCC[C@H]1C(=O)N[C@H](C(=O)O)CCCNC(N)=N)=O)([C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC([C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](COC(=O)CCCCCCC)NC(=O)[C@H](CO)NC(=O)CN)CC1C=CC=CC=1)=O)CC1NC=NC=1)=O
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| InChi Key |
GKDHXLGLEXRRSB-MVILVGDSSA-N
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| InChi Code |
InChI=1S/C142H237N43O40/c1-8-9-10-11-15-45-114(197)225-76-103(181-130(213)100(73-186)162-111(192)71-148)132(215)177-98(69-82-32-13-12-14-33-82)128(211)176-97(68-79(4)5)127(210)180-102(75-188)138(221)183-64-29-42-105(183)134(217)171-92(50-55-113(195)196)124(207)178-99(70-83-72-156-77-159-83)129(212)170-90(47-52-109(150)190)123(206)165-84(34-16-21-56-143)117(200)160-80(6)115(198)164-89(46-51-108(149)189)122(205)167-88(39-26-61-157-141(152)153)119(202)166-86(36-18-23-58-145)118(201)169-91(49-54-112(193)194)125(208)179-101(74-187)131(214)168-87(37-19-24-59-146)120(203)172-93(38-20-25-60-147)136(219)185-66-31-44-107(185)139(222)184-65-30-41-104(184)133(216)161-81(7)116(199)163-85(35-17-22-57-144)121(204)175-96(67-78(2)3)126(209)173-94(48-53-110(151)191)137(220)182-63-28-43-106(182)135(218)174-95(140(223)224)40-27-62-158-142(154)155/h12-14,32-33,72,77-81,84-107,186-188H,8-11,15-31,34-71,73-76,143-148H2,1-7H3,(H2,149,189)(H2,150,190)(H2,151,191)(H,156,159)(H,160,200)(H,161,216)(H,162,192)(H,163,199)(H,164,198)(H,165,206)(H,166,202)(H,167,205)(H,168,214)(H,169,201)(H,170,212)(H,171,217)(H,172,203)(H,173,209)(H,174,218)(H,175,204)(H,176,211)(H,177,215)(H,178,207)(H,179,208)(H,180,210)(H,181,213)(H,193,194)(H,195,196)(H,223,224)(H4,152,153,157)(H4,154,155,158)/t80-,81-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-/m0/s1
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| Chemical Name |
(4S)-4-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-hydroxypropanoyl]amino]-3-octanoyloxypropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]amino]-5-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-6-amino-1-[(2S)-2-[(2S)-2-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-5-amino-1-[(2S)-2-[[(1S)-4-carbamimidamido-1-carboxybutyl]carbamoyl]pyrrolidin-1-yl]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O: 100 mg/mL (31.38 mM)
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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 | 0.3138 mL | 1.5690 mL | 3.1381 mL | |
| 5 mM | 0.0628 mL | 0.3138 mL | 0.6276 mL | |
| 10 mM | 0.0314 mL | 0.1569 mL | 0.3138 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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