| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The biological effects of Locustatachykinin I are mediated through specific insect tachykinin receptors that are homologous to vertebrate tachykinin receptors (TKRs). Characterization studies have involved functional expression in stable Drosophila Schneider 2 cell lines to analyze receptor binding and activation. The peptide shows high affinity for its cognate receptors and exhibits sequence homology that suggests conserved receptor interactions across species. Additionally, it has been shown to have receptor activity for the α1-adrenergic receptor in ganglia cells, which can regulate nerve impulses. The peptide's interactions with multiple receptor systems underscore its complex role in insect neurophysiology.
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| ln Vitro |
In vitro studies have demonstrated that Locustatachykinin I exhibits significant biological activities. It has been shown to have a diuretic action in insect Malpighian tubules, as demonstrated by its effects on fluid secretion in isolated tubule preparations. The peptide also modulates neurogenic inflammation and muscle contraction in insect models. Its anti-inflammatory properties may be due to its inhibition of proctolin, a peptide hormone that causes inflammation. The peptide's activity is typically assessed through fluid secretion assays in isolated Malpighian tubules, where it stimulates secretion in a dose-dependent manner, confirming its role as a diuretic hormone in insects.
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| ln Vivo |
In vivo studies have focused on the diuretic action of Locustatachykinin I in locusts, analyzing its effects on fluid secretion in Malpighian tubules. The peptide modulates physiological processes in the insect nervous system, including neurotransmission and muscle contraction. Its anti-inflammatory properties have also been observed in vivo through inhibition of proctolin-mediated inflammation. These studies have established locustatachykinin I as a key regulator of fluid balance and neurophysiology in insects, with potential applications in understanding insect physiology and developing novel pest control strategies.
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| Enzyme Assay |
Typical non-cell-based assays for tachykinin-related peptides involve radioligand binding studies using membrane preparations from cells expressing cloned tachykinin receptors. Competitive binding experiments are performed with increasing concentrations of the peptide and a fixed concentration of a radiolabeled tracer, with binding affinity (Ki) determined by nonlinear regression analysis of displacement curves. Assays are conducted in buffer containing protease inhibitors at room temperature for 60-90 minutes, followed by rapid filtration through glass fiber filters and scintillation counting. These cell-free systems allow for precise characterization of receptor-ligand interactions without interference from cellular metabolism.
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| Cell Assay |
Cellular assays for Locustatachykinin I typically involve calcium mobilization assays in cells expressing cloned insect tachykinin receptors, where peptide-induced intracellular calcium release is measured using fluorescent indicators such as Fura-2 or Fluo-4. Additionally, second messenger assays measuring inositol phosphate accumulation or cAMP levels can be employed to characterize receptor coupling and signaling pathways. Drosophila Schneider 2 cell lines have been used for functional expression studies to characterize receptor activation and signaling. These cell-based systems enable detailed analysis of receptor pharmacology and signal transduction mechanisms.
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| Animal Protocol |
In vivo experiments with Locustatachykinin I typically utilize isolated Malpighian tubules from locusts to measure fluid secretion rates. Tubules are dissected and incubated in physiological saline, and the rate of fluid secretion is measured before and after peptide application at concentrations ranging from 10⁻⁹ to 10⁻⁶ M. The effect on fluid secretion is quantified as the percentage change from baseline, demonstrating the peptide's diuretic action. These experiments have established the physiological role of locustatachykinin I as a diuretic hormone in insects and provide a robust model for studying neuropeptide function in vitro.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Locustatachykinin I are not available in the consulted sources. As a peptide, it would be expected to have poor oral bioavailability and rapid degradation by proteolytic enzymes in vivo. Peptide drugs typically have short half-lives and require parenteral administration. Studies have identified four neuropeptide-degrading enzymes in neuronal membranes of insects that inactivate tachykinin-like peptides. Metabolic stability can be enhanced through modification of the peptide sequence, such as incorporation of D-amino acids or cyclization, but such modifications have not been reported for this specific peptide.
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| Toxicity/Toxicokinetics |
Toxicological data for Locustatachykinin I are not available in the consulted sources. As an insect neuropeptide, its toxicity profile in mammals has not been extensively characterized. Peptides generally have low toxicity due to their rapid degradation to amino acids. However, potential immunogenicity and off-target effects on mammalian tachykinin receptors would need to be evaluated in preclinical safety studies if therapeutic applications were considered. Currently, the compound is used exclusively for research purposes and is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
Locustatachykinin I is exclusively a research tool for studying insect neuropeptide systems and tachykinin-related signaling. It has no clinical applications or approved drug status. The peptide is valuable for understanding the evolutionary conservation of tachykinin signaling across species and for investigating insect physiology. Research applications include studies of diuretic regulation, neurogenic inflammation, and muscle contraction in insects. It is not intended for human therapeutic use and is available from commercial suppliers for laboratory research purposes only.
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| Molecular Formula |
C43H63N13O11
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|---|---|
| Molecular Weight |
938.04
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| Exact Mass |
937.477
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| CAS # |
126985-97-5
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| Related CAS # |
Locustatachykinin I TFA
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| PubChem CID |
195503
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| Appearance |
White to off-white solid powder
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| Density |
1.46g/cm3
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| Index of Refraction |
1.666
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| LogP |
0.446
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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 |
26
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| Heavy Atom Count |
67
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| Complexity |
1730
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N)NC(=O)CNC(=O)[C@H](CC1=CC=C(C=C1)O)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]3CCCN3C(=O)CN
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| InChi Key |
QVHUTTNZGVKOKQ-LINCNNNZSA-N
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| InChi Code |
InChI=1S/C43H63N13O11/c1-24(2)36(42(67)52-28(37(45)62)10-6-16-48-43(46)47)55-34(60)22-49-38(63)29(19-26-12-14-27(58)15-13-26)53-40(65)30(18-25-8-4-3-5-9-25)51-33(59)21-50-39(64)31(23-57)54-41(66)32-11-7-17-56(32)35(61)20-44/h3-5,8-9,12-15,24,28-32,36,57-58H,6-7,10-11,16-23,44H2,1-2H3,(H2,45,62)(H,49,63)(H,50,64)(H,51,59)(H,52,67)(H,53,65)(H,54,66)(H,55,60)(H4,46,47,48)/t28-,29-,30-,31-,32-,36-/m0/s1
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| Chemical Name |
(2S)-1-(2-aminoacetyl)-N-[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
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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) |
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 | 1.0661 mL | 5.3303 mL | 10.6605 mL | |
| 5 mM | 0.2132 mL | 1.0661 mL | 2.1321 mL | |
| 10 mM | 0.1066 mL | 0.5330 mL | 1.0661 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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