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| 1mg |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
GRP targets the gastrin-releasing peptide receptor (GRPR), a G protein-coupled receptor. It also functions as a mitogen for multiple cancers, including small-cell lung carcinoma and neuroblastoma.
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|---|---|
| ln Vitro |
Due to its small involvement in modulating pituitary hormone release, human gastrin-releasing peptide (GRP), which is a member of the bombesin-like peptide family, is not a conventional hypothalamic-pituitary regulatory hormone. Nonetheless, the mammalian brain contains GRP/bombesin-like immunoreactivity in several areas, particularly the gastrointestinal system, the hypothalamus, and the human fetal lung [1].
In vitro, GRP stimulates the proliferation of cancer cell lines that express GRPR, including small-cell lung carcinoma and neuroblastoma cells. It activates downstream signaling pathways such as MAPK and PI3K/AKT. |
| ln Vivo |
In vivo, GRP acts as a growth-modulating factor in developing lung epithelium and has been implicated in the growth of GRPR-expressing tumors. It is used as a tumor marker for small-cell lung carcinoma.
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| Enzyme Assay |
GRPR binding affinity is measured using radioligand binding assays with membranes from cells expressing GRPR. Competitive binding assays with labeled GRP or bombesin are used to determine receptor affinity and selectivity.
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| Cell Assay |
Cells expressing GRPR (e.g., small-cell lung carcinoma cell lines) are cultured and treated with GRP. Cell proliferation is measured by BrdU incorporation or MTT assay. Signaling pathway activation is assessed by Western blotting for phosphorylated kinases.
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| Animal Protocol |
Xenograft models using GRPR-expressing tumor cells in immunocompromised mice are used to evaluate tumor growth. GRP or GRPR antagonists are administered to study their effects on tumor progression. GRP levels in plasma are measured as a tumor marker.
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| ADME/Pharmacokinetics |
GRP has a short half-life in circulation due to rapid enzymatic degradation. It is a regulatory peptide rather than a therapeutic drug. Its pharmacokinetics are not extensively characterized for therapeutic use.
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| Toxicity/Toxicokinetics |
GRP itself is not toxic at physiological concentrations. However, overexpression of GRP and its receptor is associated with tumor growth and progression. GRP is not used as a therapeutic agent; it is a research tool and tumor marker.
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| References |
[1]. Dubovy SR, et al. Expression of hypothalamic neurohormones and their receptors in the human eye. Oncotarget. 2017 Jun 3.
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| Additional Infomation |
GRP is a research peptide and tumor marker with no therapeutic approval status. It is used in diagnostic assays for small-cell lung carcinoma and in research on bombesin-like peptide biology and cancer.
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| Molecular Formula |
C130H204N38O31S2
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|---|---|
| Molecular Weight |
2859.37675999999
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| Exact Mass |
2857.499
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| CAS # |
93755-85-2
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| PubChem CID |
23185015
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.672
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| LogP |
-1.4
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| Hydrogen Bond Donor Count |
36
|
| Hydrogen Bond Acceptor Count |
38
|
| Rotatable Bond Count |
86
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| Heavy Atom Count |
201
|
| Complexity |
6470
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1=CNC2C=CC=CC1=2)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N)CCSC)CC1NC=NC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)N)NC(=O)CNC(=O)[C@H](CCCNC(N)=N)NC([C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@H](O)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C(C)C)NC(=O)[C@H]([C@H](O)C)NC(=O)CNC(=O)CNC(=O)CNC(=O)[C@H](C)NC([C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC([C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)=O)=O)CC1C=CC(O)=CC=1)=O)CC1NC=NC=1
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| InChi Key |
PUBCCFNQJQKCNC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C130H204N38O31S2/c1-65(2)47-86(115(185)152-82(108(134)178)38-45-200-17)156-116(186)89(52-77-56-137-63-146-77)150-101(176)62-145-123(193)104(69(9)10)163-110(180)72(14)148-114(184)88(51-76-55-140-81-28-20-19-27-80(76)81)157-117(187)90(53-78-57-138-64-147-78)158-118(188)91(54-97(132)172)151-100(175)61-144-111(181)83(30-23-41-139-130(135)136)154-121(191)95-32-25-43-167(95)128(198)93(50-75-34-36-79(171)37-35-75)160-113(183)85(39-46-201-18)153-112(182)84(29-21-22-40-131)155-125(195)107(74(16)170)165-119(189)87(48-66(3)4)159-124(194)105(70(11)12)164-126(196)106(73(15)169)162-102(177)60-142-98(173)58-141-99(174)59-143-109(179)71(13)149-120(190)94-31-24-42-166(94)127(197)92(49-67(5)6)161-122(192)96-33-26-44-168(96)129(199)103(133)68(7)8/h19-20,27-28,34-37,55-57,63-74,82-96,103-107,140,169-171H,21-26,29-33,38-54,58-62,131,133H2,1-18H3,(H2,132,172)(H2,134,178)(H,137,146)(H,138,147)(H,141,174)(H,142,173)(H,143,179)(H,144,181)(H,145,193)(H,148,184)(H,149,190)(H,150,176)(H,151,175)(H,152,185)(H,153,182)(H,154,191)(H,155,195)(H,156,186)(H,157,187)(H,158,188)(H,159,194)(H,160,183)(H,161,192)(H,162,177)(H,163,180)(H,164,196)(H,165,189)(H4,135,136,139)
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| Chemical Name |
2-[[2-[[2-[[1-[2-[[2-[[6-amino-2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[2-[[1-[2-[[1-(2-amino-3-methylbutanoyl)pyrrolidine-2-carbonyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]amino]propanoylamino]acetyl]amino]acetyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-3-methylbutanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]hexanoyl]amino]-4-methylsulfanylbutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carbonyl]amino]-5-carbamimidamidopentanoyl]amino]acetyl]amino]-N-[1-[[1-[[1-[[1-[[2-[[1-[[1-[(1-amino-4-methylsulfanyl-1-oxobutan-2-yl)amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]butanediamide
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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, avoid exposure to moisture. |
| 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 (~34.97 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 | 0.3497 mL | 1.7486 mL | 3.4973 mL | |
| 5 mM | 0.0699 mL | 0.3497 mL | 0.6995 mL | |
| 10 mM | 0.0350 mL | 0.1749 mL | 0.3497 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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