![[Sar9,Met(O2)11]-Substance P TFA](/upload/1124/V70789.png)
| 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 |
NK1 receptor[1]
[Sar9,Met(O2)11]-Substance P TFA targets the tachykinin NK1 receptor. It is a selective agonist for this receptor. The NK1 receptor is a key player in neurokinin signaling pathways and is involved in pain modulation, stress response, and anxiety disorders. By activating NK1 receptors, the compound modulates neurokinin signaling. |
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| ln Vitro |
[Sar9,Met(O2)11]-Substance P and septide (10-100 pmol per rat, icv) are equally effective in raising heart rate (HR) and mean arterial blood pressure (MAP), although their time courses are different. Face washing and sniffing are increased dose-dependently by both agonists, but only [Sar9,Met(O2)11]-Substance P causes grooming[1].
In vitro, [Sar9,Met(O2)11]-Substance P TFA acts as a selective NK1 receptor agonist. [Sar9,Met(O2)11]-Substance P and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissimilar time-course. Its activity is typically assessed in receptor binding studies and functional assays measuring calcium mobilization or other signaling readouts. |
| ln Vivo |
In vivo, [Sar9,Met(O2)11]-Substance P TFA and septide (10-100 pmol per rat, i.c.v.) are equipotent in increasing mean arterial blood pressure (MAP) and heart rate (HR), yet they have dissimilar time-course. It has demonstrated potent biological activity, making it useful in research applications related to pain modulation, stress response, and anxiety disorders.
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| Enzyme Assay |
For non-cell-based receptor binding assays, [Sar9,Met(O2)11]-Substance P 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 [Sar9,Met(O2)11]-Substance P TFA. Fluorescence intensity is measured using a fluorescence plate reader. The increase in calcium signal compared to control wells indicates agonist activity. EC50 values are calculated from dose-response curves.
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| Animal Protocol |
For in vivo animal studies, [Sar9,Met(O2)11]-Substance P TFA can be administered to rats via intracerebroventricular (i.c.v.) injection. In models of cardiovascular regulation, its effects on mean arterial blood pressure and heart rate are assessed. In models of pain and anxiety, behavioral responses are evaluated. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
[Sar9,Met(O2)11]-Substance P TFA has a molecular weight of 1507.68 and a molecular formula of C66H101N18F3O17S. It is a selective NK1 receptor agonist. The compound should be stored according to the manufacturer's recommendations. It is for research use only and is not intended for human consumption.
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| Toxicity/Toxicokinetics |
The toxicity profile of [Sar9,Met(O2)11]-Substance P TFA has not been extensively reported. As an NK1 receptor agonist, 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 |
[Sar9,Met(O2)11]-Substance P TFA (CAS 2828433-10-7) is a selective tachykinin NK1 receptor agonist. It is a selective agonist for the tachykinin NK1 receptor, a key player in neurokinin signaling pathways. It has demonstrated potent biological activity and is used in research related to pain modulation, stress response, and anxiety disorders. It is available for research purposes only.
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| Molecular Formula |
C66H101F3N18O17S
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|---|---|
| Molecular Weight |
1507.67876410484
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| Exact Mass |
1506.726
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| CAS # |
2828433-10-7
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| Related CAS # |
[Sar9,Met(O2)11]-Substance P;110880-55-2
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| PubChem CID |
163335260
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
23
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| Rotatable Bond Count |
42
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| Heavy Atom Count |
105
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| Complexity |
2970
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C(F)(F)(F)C(=O)O.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)N[C@H](C(=O)N(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N)CCS(=O)(=O)C)CC1C=CC=CC=1)CC1C=CC=CC=1)(=O)[C@H](CCCCN)NC([C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(N)=N)=O
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| InChi Key |
VDZDOTCGVUBCPG-LYQMAKBCSA-N
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| InChi Code |
InChI=1S/C64H100N18O15S.C2HF3O2/c1-38(2)34-46(57(89)74-42(54(69)86)28-33-98(4,96)97)73-53(85)37-80(3)62(94)48(36-40-18-9-6-10-19-40)79-58(90)47(35-39-16-7-5-8-17-39)78-56(88)43(24-26-51(67)83)75-55(87)44(25-27-52(68)84)76-59(91)50-23-15-32-82(50)63(95)45(21-11-12-29-65)77-60(92)49-22-14-31-81(49)61(93)41(66)20-13-30-72-64(70)71;3-2(4,5)1(6)7/h5-10,16-19,38,41-50H,11-15,20-37,65-66H2,1-4H3,(H2,67,83)(H2,68,84)(H2,69,86)(H,73,85)(H,74,89)(H,75,87)(H,76,91)(H,77,92)(H,78,88)(H,79,90)(H4,70,71,72);(H,6,7)/t41-,42-,43-,44-,45-,46-,47-,48-,49-,50-;/m0./s1
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| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-1-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-N-[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methylsulfonyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]-methylamino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1,5-dioxopentan-2-yl]pentanediamide;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: 100 mg/mL (66.33 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (33.16 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 | 0.6633 mL | 3.3164 mL | 6.6327 mL | |
| 5 mM | 0.1327 mL | 0.6633 mL | 1.3265 mL | |
| 10 mM | 0.0663 mL | 0.3316 mL | 0.6633 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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