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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
LGnRH-III targets the mammalian GnRH receptor (also known as LHRH receptor). It acts as a weak agonist at this receptor, exerting a direct antiproliferative effect on cancer cells. The specificity of LGnRH-III for the mammalian LHRH receptor has been demonstrated by blocking the receptor with the LHRH antagonist MI-1544.
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| ln Vitro |
In vitro, LGnRH-III demonstrates a direct antiproliferative effect on cancer cells. It acts as a weak GnRH receptor agonist. The peptide dose-dependently inhibits cancer cell proliferation through modulation of hormonal pathways. Detailed IC₅0 values for its antiproliferative activity are not extensively documented in the available literature.
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| ln Vivo |
In vivo activity data for LGnRH-III are not extensively characterized. As a GnRH receptor agonist with antitumor properties, the compound is expected to modulate gonadotropin secretion and exert antiproliferative effects in vivo. Further in vivo studies in appropriate tumor models would be needed to fully characterize its pharmacokinetic and efficacy profile.
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| Enzyme Assay |
The in vitro receptor binding assay for LGnRH-III uses membrane preparations from cells expressing mammalian GnRH receptors. Competitive binding is performed using radiolabeled GnRH agonists in the presence of varying concentrations of LGnRH-III. Receptor specificity is confirmed by blocking with the LHRH antagonist MI-1544. Bound radioactivity is measured, and binding affinities are calculated from displacement curves.
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| Cell Assay |
For in vitro cell-based assays, cancer cell lines expressing GnRH receptors are cultured and treated with LGnRH-III at various concentrations. Cell proliferation is measured using MTT, CellTiter-Glo, or direct cell counting. Antiproliferative effects are assessed by comparing treated cells to vehicle controls. Experiments are typically performed in triplicate under standard culture conditions (37degC, 5% CO2).
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| Animal Protocol |
In vivo animal studies for LGnRH-III would typically involve xenograft mouse models using GnRH receptor-positive cancer cell lines. Tumor-bearing mice are administered LGnRH-III via subcutaneous or intraperitoneal injection at various doses. Tumor volume is measured periodically using calipers, and tumor growth inhibition is assessed relative to vehicle-treated controls. At study termination, tumors are harvested for histopathological and molecular analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LGnRH-III are not extensively documented. As a peptide with molecular formula C₅₉H₇4N1₈O14 and molecular weight approximately 1211.3, it has limited oral bioavailability and is typically administered via injection. The compound is soluble in aqueous buffers and DMSO. Storage at -20degC is recommended for long-term preservation. Further detailed PK parameters would require dedicated studies.
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| Toxicity/Toxicokinetics |
Toxicological data for LGnRH-III are not well characterized in the public domain. As a research peptide, standard safety precautions should be observed. The compound is for laboratory use only and not intended for human therapeutic applications. Peptide-based research compounds generally have favorable safety profiles but may have immunogenicity risks. Comprehensive toxicity profiling would be required for therapeutic development.
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| References | |
| Additional Infomation |
LGnRH-III, lamprey (CAS# 147859-97-0) is a GnRH isoform isolated from the sea lamprey. It is a weak GnRH receptor agonist with antitumor activities. The peptide is used in cancer research to study hormonal pathways and therapeutic strategies targeting GnRH receptors. It is not approved for clinical use and is strictly for laboratory research purposes.
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| Molecular Formula |
C59H75N19O13
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|---|---|
| Molecular Weight |
1258.3463
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| Exact Mass |
1258.56
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| CAS # |
147859-97-0
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| PubChem CID |
16197823
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| Appearance |
White to off-white solid powder
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| LogP |
1.021
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| Hydrogen Bond Donor Count |
17
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
91
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| Complexity |
2610
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C1C[C@H](N(C1)C(=O)[C@H](CCCCN)NC(=O)[C@H](CC2=CNC3=CC=CC=C32)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC4=CN=CN4)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CN=CN7)NC(=O)[C@@H]8CCC(=O)N8)C(=O)NCC(=O)N
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| InChi Key |
RTASYRSYWSLWJV-CSYZDTNESA-N
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| InChi Code |
InChI=1S/C59H74N18O14/c60-16-6-5-12-40(59(91)77-17-7-13-47(77)58(90)66-27-48(61)79)70-52(84)41(18-31-23-64-37-10-3-1-8-35(31)37)72-56(88)45(22-50(81)82)75-55(87)44(21-34-26-63-30-68-34)74-57(89)46(28-78)76-53(85)42(19-32-24-65-38-11-4-2-9-36(32)38)71-54(86)43(20-33-25-62-29-67-33)73-51(83)39-14-15-49(80)69-39/h1-4,8-11,23-26,29-30,39-47,64-65,78H,5-7,12-22,27-28,60H2,(H2,61,79)(H,62,67)(H,63,68)(H,66,90)(H,69,80)(H,70,84)(H,71,86)(H,72,88)(H,73,83)(H,74,89)(H,75,87)(H,76,85)(H,81,82)/t39-,40-,41-,42-,43-,44-,45-,46-,47-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S)-1-[[(2S)-6-amino-1-[(2S)-2-[(2-amino-2-oxoethyl)carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-[[(2S)-2-[[(2S)-3-hydroxy-2-[[(2S)-2-[[(2S)-3-(1H-imidazol-5-yl)-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-4-oxobutanoic 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, 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 : ~50 mg/mL (~39.70 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (79.41 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7947 mL | 3.9735 mL | 7.9469 mL | |
| 5 mM | 0.1589 mL | 0.7947 mL | 1.5894 mL | |
| 10 mM | 0.0795 mL | 0.3973 mL | 0.7947 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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