| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Bombesin receptor. Litorin is a bombesin receptor agonist. The compound activates bombesin receptors to stimulate smooth muscle contraction, gastrin release, gastric acid secretion, and pancreatic secretion.
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| ln Vitro |
99mTc-Litorin was created to image tumors overexpressing the gastrin-releasing peptide receptor (GRP-R) without requiring surgery [1]. [D-Phe1,Leu8,9]With a Ki of 5.1 nM, lexirin prevents 125I-[Tyr4]BN from attaching to mouse Swiss 3T3 cells[2]. With an EC50 of 2.3 nM, ligand promotes the incorporation of 3H-thymidine in mouse Swiss 3T3 cells [2].
Litorin is a bombesin receptor agonist. It stimulates smooth muscle contraction, gastrin secretion, gastric acid secretion, and pancreatic secretion. The peptide shows potent agonistic activity at bombesin receptors. |
| ln Vivo |
In in vivo tests, Litorin promotes smooth muscle contraction, stimulates gastrin, gastric acid, and pancreatic secretion, and inhibits nutrition [2].
Litorin suppresses nutrient intake in vivo. It stimulates smooth muscle contraction, gastrin, gastric acid, and pancreatic secretion in animal models. The peptide has been used to study bombesin receptor physiology and gastrointestinal function. Detailed in vivo efficacy has been reported in gastrointestinal and metabolic studies. |
| Enzyme Assay |
Bombesin receptor binding assay: Membranes from cells expressing bombesin receptors are incubated with varying concentrations of Litorin and a radiolabeled bombesin receptor ligand in binding buffer at room temperature for 60–90 min. Nonspecific binding is determined with excess unlabeled ligand. Bound radioactivity is measured by filtration. Binding affinity (Ki or Kd) is calculated.
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| Cell Assay |
Functional receptor activation assay: Cells expressing bombesin receptors are treated with Litorin at varying concentrations. Receptor-mediated signaling (e.g., intracellular calcium mobilization or inositol phosphate accumulation) is measured. EC50 values for receptor activation are calculated from dose-response curves.
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| Animal Protocol |
Smooth muscle contraction assay: Isolated smooth muscle preparations (e.g., guinea pig ileum or rat stomach strips) are mounted in organ baths and treated with Litorin at varying concentrations. Muscle contraction is measured isotonically or isometrically. The potency of Litorin-induced contraction is calculated.
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| ADME/Pharmacokinetics |
Litorin has a CAS number of 55749-97-8. It is an amphibian bombesin peptide derivative. The peptide is a bombesin receptor agonist. Comprehensive PK parameters for the peptide remain to be characterized.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published. Litorin is for research use only. Standard laboratory safety practices should be followed when handling this peptide. As a bombesin receptor agonist, potential effects on gastrointestinal and metabolic function should be considered.
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| References |
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| Additional Infomation |
Litorin is an amphibian bombesin peptide derivative and a bombesin receptor agonist. It stimulates smooth muscle contraction, gastrin, gastric acid, and pancreatic secretion, and suppresses nutrient intake in vivo. Litorin is a research tool for studying bombesin receptor physiology. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C51H68N14O11S
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|---|---|
| Molecular Weight |
1085.23782
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| Exact Mass |
1084.49
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| CAS # |
55749-97-8
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| PubChem CID |
5486808
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| Appearance |
White to off-white solid powder
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| Density |
1.34 g/cm3
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| Boiling Point |
1693.3ºC at 760 mmHg
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| Flash Point |
977.9ºC
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| Index of Refraction |
1.615
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| LogP |
2.743
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
30
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| Heavy Atom Count |
77
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| Complexity |
2100
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C[C@@H](C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@@H]5CCC(=O)N5
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| InChi Key |
OHCNRADJYUSTIV-FPNHNIPFSA-N
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| InChi Code |
InChI=1S/C51H68N14O11S/c1-27(2)43(51(76)56-25-42(68)60-39(22-31-24-54-26-57-31)50(75)63-37(20-29-10-6-5-7-11-29)49(74)61-34(44(53)69)18-19-77-4)65-45(70)28(3)58-48(73)38(21-30-23-55-33-13-9-8-12-32(30)33)64-47(72)36(14-16-40(52)66)62-46(71)35-15-17-41(67)59-35/h5-13,23-24,26-28,34-39,43,55H,14-22,25H2,1-4H3,(H2,52,66)(H2,53,69)(H,54,57)(H,56,76)(H,58,73)(H,59,67)(H,60,68)(H,61,74)(H,62,71)(H,63,75)(H,64,72)(H,65,70)/t28-,34-,35-,36-,37-,38-,39-,43-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-5-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]-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanediamide
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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) |
DMSO : ~100 mg/mL (~92.15 mM)
H2O : ~2 mg/mL (~1.84 mM ) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9215 mL | 4.6073 mL | 9.2146 mL | |
| 5 mM | 0.1843 mL | 0.9215 mL | 1.8429 mL | |
| 10 mM | 0.0921 mL | 0.4607 mL | 0.9215 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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