| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Substance P(1-7) TFA targets the neurokinin-1 (NK1) receptor pathway. It is a fragment of substance P, which is the endogenous ligand for the NK1 receptor. It gives depressor and bradycardic effects when applied to the nucleus tractus solitarius. It is found to act as a very potent antagonist against the SP-induced responses and is formed locally in the nigra after SP injection.
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| ln Vitro |
In vitro, Substance P(1-7) TFA is a fragment of the neuropeptide, substance P (SP). It gives depressor and bradycardic effects when applied to the nucleus tractus solitarius. It is found to act as a very potent antagonist against the SP-induced responses. It is thought that Substance P(1-7) endogenously modulates SP activity.
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| ln Vivo |
Following SP injection, substance P(1–7) is shown to develop locally in the nigra and to operate as a very powerful antagonist against the reactions elicited by SP. It has been suggested that Substance P(1–7) regulates SP activities endogenously[1]. When Substance P(1-7) (1.0-4.0 pM) is injected concurrently with SP or SP(5-11) (0.1 nM), the unpleasant behaviors caused by SP or SP(5-11) are greatly reduced. These findings suggest that endogenously produced SP(1–7) may be able to influence how SP or SP(5–11) behave in the spinal cord[2].
In vivo, Substance P(1-7) TFA gives depressor and bradycardic effects when applied to the nucleus tractus solitarius. It is formed locally in the nigra after SP injection. It is thought that Substance P(1-7) endogenously modulates SP activity. However, comprehensive in vivo efficacy data from published literature are limited. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Substance P(1-7) TFA can be evaluated using membrane preparations from cells expressing human NK1 receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [3H]-Substance P. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled Substance P. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing human NK1 receptors are cultured in appropriate media. For functional assays, calcium mobilization is measured using fluorescent calcium indicators. Cells are loaded with the dye and treated with various concentrations of Substance P(1-7) TFA in the presence of Substance P. Fluorescence intensity is measured using a fluorescence plate reader. The reduction in calcium signal compared to control indicates antagonist activity. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, Substance P(1-7) TFA can be administered to rodents via microinjection into the nucleus tractus solitarius. In models of cardiovascular regulation, its effects on blood pressure and heart rate are assessed. In models of pain, its effects on nociceptive responses are evaluated. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
Substance P(1-7) TFA has a molecular weight of 1014.06 and a molecular formula of C43H66F3N13O12. The sequence is Arg-Pro-Lys-Pro-Gln-Gln-Phe (RPKPQQF). The compound should be stored as a powder at -80°C for up to 2 years or in solvent at -80°C for 6 months. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of Substance P(1-7) TFA has not been extensively reported. As a fragment of substance P, potential adverse effects may include modulation of neurokinin signaling. The compound is for research use only and is not intended for human consumption. Standard safety precautions should be observed when handling the compound.
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| References | |
| Additional Infomation |
Substance P(1-7) TFA (CAS 2828433-22-1) is a fragment of the neuropeptide, substance P (SP). It gives depressor and bradycardic effects when applied to the nucleus tractus solitarius. It is found to act as a very potent antagonist against the SP-induced responses and is formed locally in the nigra after SP injection. It is available for research purposes only.
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| Molecular Formula |
C43H66F3N13O12
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|---|---|
| Molecular Weight |
1014.06
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| Exact Mass |
1013.49
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| CAS # |
2828433-22-1
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| Related CAS # |
Substance P(1-7);68060-49-1
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| PubChem CID |
134694976
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
27
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| Heavy Atom Count |
71
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| Complexity |
1760
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C(N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@H](C(=O)O)CC1C=CC=CC=1)(=O)[C@H](CCCCN)NC([C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(N)=N)=O.C(F)(F)(F)C(=O)O
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| InChi Key |
NGJNGAVSGJSPNQ-OSSAIMHMSA-N
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| InChi Code |
InChI=1S/C41H65N13O10.C2HF3O2/c42-19-5-4-12-28(51-37(60)30-13-7-21-53(30)38(61)25(43)11-6-20-48-41(46)47)39(62)54-22-8-14-31(54)36(59)50-27(16-18-33(45)56)34(57)49-26(15-17-32(44)55)35(58)52-29(40(63)64)23-24-9-2-1-3-10-24;3-2(4,5)1(6)7/h1-3,9-10,25-31H,4-8,11-23,42-43H2,(H2,44,55)(H2,45,56)(H,49,57)(H,50,59)(H,51,60)(H,52,58)(H,63,64)(H4,46,47,48);(H,6,7)/t25-,26-,27-,28-,29-,30-,31-;/m0./s1
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| Chemical Name |
(2S)-2-[[(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoic acid;2,2,2-trifluoroacetic 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 (49.31 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (98.61 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 | 0.9861 mL | 4.9307 mL | 9.8613 mL | |
| 5 mM | 0.1972 mL | 0.9861 mL | 1.9723 mL | |
| 10 mM | 0.0986 mL | 0.4931 mL | 0.9861 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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