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| Targets |
Senktide targets the tachykinin neurokinin-3 (NK3) receptor, a G protein-coupled receptor that is activated by the neuropeptide neurokinin B. NK3 receptors are expressed in the central nervous system, where they play a critical role in modulating neurotransmission and neuroendocrine functions. Senktide is a potent and selective agonist of the NK3 receptor. It exhibits a less potent effect on the NK1 receptor (EC50 = 35 µM) and no effect on the NK2 receptor. By binding to and activating NK3 receptors, Senktide modulates the activity of dopamine neurons and other neuronal populations, influencing various physiological processes.
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| ln Vitro |
In the substantia nigra pars compacta, 24 out of 31 dopaminergic neurons were stimulated by the chosen NK3 agonist Senktide in a concentration-dependent manner. The range of effective concentration ranges from 3 to 3000 nm. Senktide's average EC50 is 41.2±9 nm (n=5)[2].
In vitro, Senktide has been shown to directly excite dopaminergic neurons in the substantia nigra pars compacta. In electrophysiological studies, Senktide excites 24 of 31 dopaminergic neurons in a concentration-dependent manner. It enhances dopaminergic function by activating NK3 receptors. As a NK3 receptor agonist, it is used in cell-based assays to study the signaling pathways downstream of NK3 receptor activation, such as calcium mobilization and inositol phosphate accumulation. Its selectivity for NK3 over NK1 and NK2 receptors makes it a valuable tool for dissecting the specific functions of the NK3 receptor. |
| ln Vivo |
The total circulation distance increased dose-alarm following an intracardiac vein injection of Senktide (F6,72=6.344, P<0.001). Comparing this rise to the creative substance treatment group, it obtained statistical significance (0.06 nmol or higher). In a single experiment, 0.1 nmol Senktide caused a significant and dose-dependent reduction in tachykinin NK3 receptor antagonists when tested in parallel with talnetant (30 mg/kg) and SB222200 (30 mg/kg). Oxanetan did not cause a significant reduction in tachykinin NK3 receptor antagonists, but Senktide induced an increase in locomotor activity (F7,78=10.32, P<0.00)1). On the other hand, osanitan did considerably lower activity when evaluated with a different vehicle (tetrahydrofuranose and vitamin E) in comparison to gerbils given with sensktide (F2,30=10.10, P<0.001)[1].
In vivo, Senktide induces locomotor activity when administered centrally. Intracranial injection of Senktide has been shown to induce locomotor activity, which is attributed to the activation of NK3 receptors and subsequent modulation of dopaminergic function. In a study on Japanese Black cattle, Senktide decreased core temperature, demonstrating its effects on thermoregulation. These in vivo studies confirm that Senktide is a potent NK3 receptor agonist that can modulate behavior and physiological functions, making it a valuable tool for studying the role of NK3 receptors in the brain. |
| Enzyme Assay |
The in vitro assays for Senktide measure its binding to the NK3 receptor and its ability to activate NK3 receptor-mediated signaling. Receptor binding assays are performed using membranes from cells expressing the NK3 receptor and a radiolabeled ligand. Senktide's affinity (Ki) for the receptor can be determined from competition binding curves. Functional assays measure the activation of downstream signaling pathways, such as calcium mobilization. Cells expressing NK3 receptors are loaded with a calcium-sensitive dye and treated with Senktide, and the increase in intracellular calcium is measured. The EC50 for receptor activation is determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for Senktide are conducted using cells expressing the NK3 receptor. A common assay is the measurement of intracellular calcium mobilization using a fluorescent calcium indicator. Cells are treated with Senktide, and the fluorescence signal is measured in real-time using a plate reader or fluorescence microscope. The EC50 is determined from the dose-response curve. Another assay is the measurement of inositol phosphate accumulation, as NK3 receptors are Gq-coupled and activate phospholipase C. These cell-based assays confirm that Senktide is a potent agonist of the NK3 receptor and provide data on its potency and efficacy.
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| Animal Protocol |
In vivo animal experiments for Senktide are conducted to study the effects of NK3 receptor activation on behavior and physiology. In a typical study, Senktide is administered by intracranial injection or intracerebroventricular (icv) infusion. The effects on locomotor activity are assessed by measuring the distance traveled or the number of movements in an open field test. In studies on thermoregulation, Senktide is administered, and core body temperature is monitored. These experiments are essential for understanding the role of NK3 receptors in the central nervous system and for validating the receptor as a potential therapeutic target for neurological and psychiatric disorders.
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| ADME/Pharmacokinetics |
Senktide has a molecular weight of 841.97 g/mol and a molecular formula of C40H55N7O11S. It is a white powder. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized, as the compound is primarily used in vitro and for acute in vivo studies. It is a peptide and is typically administered by injection rather than orally. Stability in solution may be limited; therefore, it should be stored as a dry powder.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Senktide is not provided in standard product descriptions. As a peptide, it is generally considered to have low toxicity, but its specific toxicity profile has not been extensively studied. It is a research compound and is not intended for human or veterinary use. In in vivo studies, it is administered at doses that are effective for modulating behavior without causing overt toxicity. As with all research chemicals, standard laboratory safety precautions should be followed when handling Senktide. Its use is limited to research applications.
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| References |
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| Additional Infomation |
See also: Natalizumab (note moved to).
Senktide is a research compound and is not approved for any clinical or therapeutic use. It is a potent and selective agonist of the tachykinin NK3 receptor. It exhibits a less potent effect on the NK1 receptor (EC50 = 35 µM) and no effect on the NK2 receptor. Senktide is used as a research tool to study the role of NK3 receptors in the central nervous system, particularly in modulating neurotransmission and neuroendocrine functions. It causes direct excitation of dopamine neurons and enhances dopaminergic function. Its mechanism of action involves binding to and activating NK3 receptors, which are G protein-coupled receptors that modulate neuronal activity. |
| Molecular Formula |
C40H55N7O11S
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| Molecular Weight |
841.970000000001
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| Exact Mass |
841.368
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| CAS # |
106128-89-6
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| PubChem CID |
108147
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| Appearance |
White to off-white solid powder
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| Density |
1.29 g/cm3
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| Boiling Point |
1262.6ºC at 760 mmHg
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| Flash Point |
717.4ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.579
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| LogP |
2.99
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
26
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| Heavy Atom Count |
59
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| Complexity |
1450
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| Defined Atom Stereocenter Count |
5
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)CNC(=O)[C@H](CC1=CC=CC=C1)N(C)C(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(=O)O)NC(=O)CCC(=O)O
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| InChi Key |
HMHYXLVEFVGOPM-QKUYTOGTSA-N
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| InChi Code |
InChI=1S/C40H55N7O11S/c1-24(2)19-28(37(55)45-27(36(41)54)17-18-59-4)44-33(49)23-42-39(57)31(21-26-13-9-6-10-14-26)47(3)40(58)30(20-25-11-7-5-8-12-25)46-38(56)29(22-35(52)53)43-32(48)15-16-34(50)51/h5-14,24,27-31H,15-23H2,1-4H3,(H2,41,54)(H,42,57)(H,43,48)(H,44,49)(H,45,55)(H,46,56)(H,50,51)(H,52,53)/t27-,28-,29-,30-,31-/m0/s1
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| Chemical Name |
(3S)-4-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-1-oxo-3-phenylpropan-2-yl]-methylamino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(3-carboxypropanoylamino)-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) |
DMSO : ~50 mg/mL (~59.38 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.97 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 (2.97 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1877 mL | 5.9385 mL | 11.8769 mL | |
| 5 mM | 0.2375 mL | 1.1877 mL | 2.3754 mL | |
| 10 mM | 0.1188 mL | 0.5938 mL | 1.1877 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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