| 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 |
NK-1 tachykinin receptor. Substance P (5-11) TFA binds to the NK-1 receptor, which is the primary receptor for the parent neuropeptide Substance P. This binding initiates downstream signaling cascades involved in pain transmission, neuroinflammation, and smooth muscle contraction.
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| ln Vitro |
[3H]Substance P(5-11) TFA TFA is taken up when it is incubated with a fraction of rabbit brain that has been enriched in glial cells. Substance P is hydrolyzed into Substance P(5-11) TFA TFA upon release from nerve terminals. This high affinity absorption process may be crucial in stopping Substance P's synaptic function, as it accumulates inside glial cells and nerve terminals.
When a fraction from rabbit brain enriched in glial cells was incubated with [3H]Substance P (5-11), an uptake of the radiolabeled heptapeptide was observed. This suggests that after substance P is released from nerve terminals and hydrolyzed into the C-terminal heptapeptide (5-11), it is accumulated into glial cells and nerve terminals via a high-affinity uptake mechanism. |
| ln Vivo |
In vivo, Substance P (5-11) is the major biologically active metabolite of Substance P. The high-affinity uptake mechanism for the 5-11 heptapeptide may play an important role in terminating the synaptic action of Substance P following its release. This makes Substance P (5-11) an important molecule for studying neuropeptide inactivation and recycling.
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| Enzyme Assay |
Receptor binding assay: Membranes prepared from cells expressing NK-1 receptors are incubated with [3H]Substance P (5-11) TFA (0.1-10 nM) and increasing concentrations of unlabeled Substance P (5-11) TFA (0-1000 nM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl2, 0.1% BSA) for 60 min at 25degC. Non-specific binding is determined with 10 uM unlabeled Substance P. Bound radioactivity is separated by filtration through GF/B filters, and IC50 is calculated by non-linear regression.
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| Cell Assay |
Uptake assay: A fraction from rabbit brain enriched in glial cells is prepared by density gradient centrifugation. The cells are incubated with [3H]Substance P (5-11) TFA (1-100 nM) in the presence or absence of unlabeled peptide for 15-60 min at 37degC. The reaction is terminated by rapid filtration, and the radioactivity retained on the filters is measured by scintillation counting. A high-affinity, saturable uptake component is identified.
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| Animal Protocol |
Not directly applicable. Substance P (5-11) TFA is a research tool for studying substance P metabolism and clearance. It may be administered to rodents to study neuropeptide uptake and turnover in the brain. Brain regions are dissected, and tissue content of Substance P (5-11) is measured by LC-MS/MS to assess rates of peptide hydrolysis and internalization.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Substance P (5-11) TFA are limited. As a 7-amino acid peptide (MW 869.04 free base, TFA salt), it has a short plasma half-life (minutes) due to rapid proteolytic degradation. It is typically administered via intracerebroventricular or intrathecal injection for CNS studies. The TFA salt enhances solubility in aqueous buffers.
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| Toxicity/Toxicokinetics |
Toxicity data for Substance P (5-11) TFA are not available. As a neuropeptide fragment, it is generally non-toxic at the low concentrations used for receptor binding and uptake studies (nM to uM). It is intended for research use only and not for human therapeutic applications. Standard safety precautions for handling peptides should be observed.
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| References | |
| Additional Infomation |
Substance P (5-11) TFA is a research-grade neuropeptide fragment used to study substance P biology, neurokinin receptors, and neuropeptide inactivation mechanisms. It is not a drug candidate and has not entered clinical trials. The sequence is QQFFGLM-NH2. For research use only. Store at -80degC for long-term stability.
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| Molecular Formula |
C41H60N10O9S.XC2HF3O2
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|---|---|
| Molecular Weight |
869.04 (free base)
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| Related CAS # |
Substance P (5-11);51165-09-4
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| Appearance |
Solid powder
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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 :~100 mg/mL
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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.) |
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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