| Size | Price | Stock | Qty |
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| 5mg |
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| 1g | |||
| Other Sizes |
| Targets |
Substance P 1-7 targets a unique, high-affinity binding site that is not recognized by NK1 ligands, with a Kd of 0.5 nM. It primarily targets neurokinin receptors, though its binding characteristics are distinct from those of the full-length Substance P. The compound's interaction with the neurokinin receptor leads to anti-inflammatory, anti-nociceptive, and anti-hyperalgesic effects. It binds to receptors in the brain and spinal cord, leading to an inhibition of glutamate release. This inhibition leads to a decrease in locomotor activity and dopamine release. The compound's unique receptor binding profile and biological effects make it a valuable tool for studying neuropeptide signaling and its role in pain, inflammation, and cardiovascular regulation.
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| ln Vitro |
In vitro studies have shown that Substance P 1-7 acts as a very potent antagonist against Substance P-induced responses. It is formed locally in the substantia nigra after SP injection, suggesting a role in modulating the effects of the parent peptide. The compound's binding sites are consistent with those expected for an SP N-terminal receptor, indicating a distinct receptor subtype or binding site. Its ability to inhibit dopamine release and glutamate release in the brain suggests significant neuromodulatory effects. The compound's anti-inflammatory, anti-nociceptive, and anti-hyperalgesic activities are mediated through its interaction with neurokinin receptors.
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| ln Vivo |
After injecting SP, substance P (1–7) was discovered to develop locally in the substantia nigra and to operate as a very strong antagonist against SP-induced reactions. Substance P (1–7) is thought by some to be an endogenous regulator of SP activity [1]. Substance P (1-7) injections at low doses (1.0-4.0 pM) given concurrently with SP or SP(5-11) injections at low doses (0.1 nM) greatly decreased the unpleasant behavior caused by SP or SP(5-11). These findings suggest that the effects of SP or SP(5–11) in the spinal cord can be modulated by endogenously produced SP(1–7) [2].
In vivo, Substance P 1-7 has been shown to have depressor and bradycardic effects when administered to the nucleus tractus solitarius, indicating its role in cardiovascular regulation. It modulates opioid signaling, induces gastric mucosal protection, and inhibits retinal apoptosis in various animal models. The compound's anti-nociceptive and anti-hyperalgesic actions suggest potential therapeutic applications in pain management. Its ability to inhibit dopamine release in the brain suggests potential applications in neurological and psychiatric disorders. However, comprehensive in vivo efficacy and safety studies are needed to fully evaluate its therapeutic potential. |
| Enzyme Assay |
In vitro non-cell receptor binding assays for Substance P 1-7 typically involve radioligand binding studies using membrane preparations from cells expressing neurokinin receptors or brain tissue. The compound's affinity (Kd) is determined by competitive displacement of a radiolabeled ligand such as [³H]Substance P. The binding characteristics of SP(1-7) are consistent with those expected for an SP N-terminal receptor, indicating a distinct binding site. Functional assays using membrane preparations can measure the compound's effects on receptor-mediated signaling, such as GTPγS binding. These assays provide quantitative data on the compound's direct interactions with its molecular targets.
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| Cell Assay |
In vitro cell-based assays for Substance P 1-7 use neuronal cell lines or primary neurons to study its effects on neurotransmitter release and signaling. Cells are treated with varying concentrations of SP(1-7), and parameters such as dopamine release, glutamate release, and intracellular calcium levels are measured. The compound's effects on neurokinin receptor signaling are assessed by measuring downstream signaling pathways, such as cAMP accumulation or MAPK activation. The anti-inflammatory effects of the compound can be studied in immune cells, where the production of inflammatory cytokines is measured. These studies help to characterize the compound's cellular mechanism of action.
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| Animal Protocol |
In vivo animal studies for Substance P 1-7 employ various models to study its effects on pain, inflammation, cardiovascular regulation, and neurological function. For pain studies, standard models such as the hot plate test, tail flick test, or formalin test are used. The compound is administered via intracerebroventricular, intrathecal, or systemic routes, and pain responses are measured. For cardiovascular studies, the compound is administered to the nucleus tractus solitarius, and blood pressure and heart rate are monitored. For neurological studies, the compound's effects on dopamine release and locomotor activity are assessed in rodent models. Pharmacokinetic studies in these models provide information about the compound's distribution and metabolism.
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| ADME/Pharmacokinetics |
Substance P 1-7 has a molecular weight of 900.04 g/mol and a molecular formula of C₄₁H₆₅N₁₃O₁₀. It has the amino acid sequence Arg-Pro-Lys-Pro-Gln-Gln-Phe. The compound should be stored at -20°C and kept tightly closed. It is available as a ≥97% pure (HPLC) solid powder for research applications. As a peptide, Substance P 1-7 is expected to have poor oral bioavailability and a short half-life in vivo due to rapid degradation by peptidases. It is typically administered by injection for research purposes. Detailed pharmacokinetic parameters have not been extensively characterized.
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| Toxicity/Toxicokinetics |
The toxicity profile of Substance P 1-7 has not been comprehensively evaluated in published studies. As an endogenous peptide fragment, it is generally considered to have low toxicity at physiological concentrations. The compound's anti-nociceptive and anti-inflammatory effects suggest potential therapeutic applications with a favorable safety profile. However, comprehensive toxicological studies are needed to fully evaluate its safety for therapeutic use. The compound is classified as a research reagent and is not intended for human therapeutic use without further safety evaluation. Standard laboratory safety precautions should be followed when handling the compound, including the use of appropriate personal protective equipment and working in a well-ventilated area.
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| References | |
| Additional Infomation |
Substance P 1-7 is the major bioactive N-terminal metabolite of the tachykinin neuropeptide Substance P, formed through endogenous proteolytic cleavage. It is also known as Substance P Fragment 1-7 and SP(1-7). The compound has the amino acid sequence Arg-Pro-Lys-Pro-Gln-Gln-Phe and a molecular weight of 900.04 g/mol. It exerts biological effects that are frequently opposite to those of its full-length parent peptide, including anti-nociceptive and anti-hyperalgesic actions. SP(1-7) has a unique, high-affinity binding site (Kd 0.5 nM) not recognized by NK1 ligands. The compound exhibits depressor and bradycardic effects when administered to the nucleus tractus solitarius. It has been shown to have inhibitory effects on dopamine release in the brain. Not approved for clinical use; intended for research purposes only.
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| Molecular Formula |
C41H65N13O10
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|---|---|
| Molecular Weight |
900.035900000001
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| Exact Mass |
899.498
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| CAS # |
68060-49-1
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| Related CAS # |
Substance P(1-7) TFA;2828433-22-1
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| PubChem CID |
3368303
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.917
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
27
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| Heavy Atom Count |
64
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| Complexity |
1670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(O)[C@@H](NC([C@@H](NC([C@@H](NC([C@@H]1CCCN1C([C@@H](NC([C@@H]2CCCN2C([C@@H](N)CCCNC(N)=N)=O)=O)CCCCN)=O)=O)CCC(N)=O)=O)CCC(N)=O)=O)CC3=CC=CC=C3
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| InChi Key |
KPHDBQWTCKBKIL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C41H65N13O10/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/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)
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| Chemical Name |
2-[[5-amino-2-[[5-amino-2-[[1-[6-amino-2-[[1-[2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoyl]amino]-3-phenylpropanoic 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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.1111 mL | 5.5553 mL | 11.1106 mL | |
| 5 mM | 0.2222 mL | 1.1111 mL | 2.2221 mL | |
| 10 mM | 0.1111 mL | 0.5555 mL | 1.1111 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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