![[Sar9] Substance P](/upload/1124/V29367.png)
| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Neurokinin-1 (NK1) receptor (tachykinin receptor family). The peptide also shows activity at other tachykinin receptors (NK2, NK3) with reduced affinity.
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| ln Vitro |
In vitro, [Sar9] Substance P binds to the NK1 receptor with high affinity and induces a conformational change that activates associated G-proteins, leading to downstream signaling pathways including phospholipase C activation, inositol phosphate turnover, and calcium mobilization. The sarcosine substitution at position 9 modulates its affinity and efficacy at tachykinin receptors, enabling detailed studies of receptor-ligand interactions and agonist selectivity. The peptide shows enhanced resistance to enzymatic degradation compared to native substance P.
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| ln Vivo |
In vivo, [Sar9] Substance P is used in neurochemical mapping studies to delineate the distribution and functional relevance of tachykinin receptors in various tissues. Its enhanced stability and selectivity make it suitable for in vitro and ex vivo assays, enabling researchers to quantify receptor-mediated responses with improved accuracy. The peptide has been used to study substance P-mediated biological processes in both neuronal and non-neuronal systems.
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| Enzyme Assay |
Receptor binding assays are performed using membrane preparations from cells expressing recombinant NK1 receptors. Membranes are incubated with radiolabeled [3H]-substance P or [¹2⁵I]-substance P and varying concentrations of unlabeled [Sar9] Substance P (0.01 nM to 10 microM) in binding buffer (50 mM Tris-HCl, pH 7.4, containing BSA, MnCl2, and protease inhibitors) at room temperature for 60-90 minutes. Non-specific binding is determined in the presence of excess unlabeled substance P (1 microM). Bound and free ligand are separated by rapid filtration through GF/B filters pre-soaked in polyethylenimine, followed by scintillation or gamma counting. Competitive binding curves are analyzed to calculate Ki values. Functional assays measure NK1 receptor-mediated calcium mobilization using fluorescent calcium indicators (e.g., Fluo-4) in receptor-expressing cells.
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| Cell Assay |
Cells expressing recombinant NK1 receptors (e.g., CHO, HEK-293 cells) are seeded in 96-well black-walled plates at 30,000-50,000 cells/well. After 24 hours, cells are loaded with calcium-sensitive dye (Fluo-4 AM, 2-5 microM) in HBSS buffer containing probenecid for 30-60 minutes at 37degC. Cells are washed and [Sar9] Substance P is added at concentrations ranging from 0.01 nM to 10 microM. Fluorescence intensity (excitation 485 nm, emission 525 nm) is measured in real-time using a fluorescence plate reader. EC₅0 values are calculated from dose-response curves. Alternatively, cAMP accumulation assays or beta-arrestin recruitment assays (e.g., PathHunter®) can be used to assess receptor activation and signaling pathway preference.
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| Animal Protocol |
In vivo studies typically involve administration of [Sar9] Substance P to rodents via intracerebroventricular (ICV), intrathecal (IT), or intravenous routes. Doses range from 0.1-10 nmol depending on the route and experimental endpoint. Pharmacological responses such as pain-related behaviors, neurogenic inflammation, or cardiovascular effects are measured at multiple time points post-administration. The specificity of observed effects is confirmed using NK1 receptor antagonists (e.g., aprepitant). Tissue samples may be collected for receptor occupancy studies or downstream signaling analysis (e.g., c-Fos immunohistochemistry).
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| ADME/Pharmacokinetics |
The substitution of sarcosine at position 9 confers enhanced metabolic stability to [Sar9] Substance P compared to native substance P, which is rapidly degraded by peptidases such as neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE). The peptide has a longer half-life in biological matrices, making it suitable for extended incubation periods in assay systems. Plasma protein binding and tissue distribution are consistent with other tachykinin peptide analogs. Elimination occurs via proteolytic degradation and renal clearance.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for [Sar9] Substance P. As a research peptide, it is not intended for human therapeutic use. The peptide is generally well-tolerated in animal studies at pharmacological doses. Potential adverse effects are related to its mechanism of action as an NK1 receptor agonist and may include neurogenic inflammation, pain modulation, or cardiovascular changes depending on the route of administration and dose. Standard safety precautions for handling peptides should be observed.
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| References | |
| Additional Infomation |
[Sar9] Substance P is a research tool compound and is not an approved drug. It is widely used to probe NK1 receptor pharmacology, signal transduction pathways, and the functional dissection of substance P-mediated biological processes. The peptide serves as a model for evaluating structure-activity relationships of tachykinin peptides. It is also used in the development of peptide-based assays as a calibration standard or positive control in receptor binding assays. The sequence is Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Sar-Leu-Met-NH2 (CAS 77128-75-7, MW 1361.7).
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| Molecular Formula |
C64H100N18O13S
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| Molecular Weight |
1361.6566
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| Exact Mass |
1360.74
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| CAS # |
77128-75-7
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| PubChem CID |
5049868
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| Appearance |
White to off-white solid powder
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| LogP |
4.145
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
42
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| Heavy Atom Count |
96
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| Complexity |
2660
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CMARLNZAQITWSL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C64H100N18O13S/c1-38(2)34-46(57(89)74-42(54(69)86)28-33-96-4)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/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)
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| Chemical Name |
2-[[1-[6-amino-2-[[1-[2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-N-[5-amino-1-[[1-[[1-[[2-[[1-[(1-amino-4-methylsulfanyl-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
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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) |
H2O : ≥ 50 mg/mL (~36.72 mM)
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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 | 0.7344 mL | 3.6720 mL | 7.3440 mL | |
| 5 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | |
| 10 mM | 0.0734 mL | 0.3672 mL | 0.7344 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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