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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Substance P (3-11) acetate targets the neurokinin-1 receptor (NK1R), which is a G protein-coupled receptor (GPCR) for which full-length Substance P (1-11) is the preferred endogenous ligand. The full-length SP (1-11) binds to NK1R with high affinity (Ki ~0.5-1 nM). The (3-11) fragment contains the C-terminal domain of SP that is essential for receptor activation and biological activity. It acts as an agonist at NK1R, albeit with reduced potency compared to the full-length peptide, as it lacks the N-terminal Arg-Pro-Lys residues. By activating NK1R, it triggers downstream signaling including phospholipase C, calcium mobilization, and MAPK pathways. The fragment also crosses the BBB, making it useful for central nervous system studies. It operates within the GPCR and neuropeptide signaling pathways.
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| ln Vitro |
In vitro, Substance P (3-11) acetate exhibits contractile activity on guinea pig ileum smooth muscle, a classic assay for NK1R activation. The fragment stimulates concentration-dependent contractions (EC50 typically in the range of 1-10 uM). It also promotes chemotaxis of human monocytes, as measured by Boyden chamber assay, with significant migration observed at concentrations of 1-100 uM. The peptide is less potent than full-length SP (1-11) but retains biological activity due to the essential C-terminal sequence. It can cross the BBB in in vitro models. No cytotoxicity is observed at effective concentrations. DMSO is not typically used; the peptide is dissolved in water or PBS. Positive control: full-length Substance P (1-11).
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| ln Vivo |
No detailed in vivo data are available for Substance P (3-11) acetate specifically. Based on the known pharmacology of Substance P, the (3-11) fragment is expected to induce plasma extravasation (neurogenic inflammation) and increase vascular permeability when administered intradermally or intravenously. Because it can cross the BBB, it may also induce behavioral effects (e.g., scratching, grooming) following central administration. However, the fragment is less potent than the full-length peptide. In vivo studies would measure NK1R-mediated responses such as paw edema, pain behavior, or cytokine release. For research use only.
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| Enzyme Assay |
For non-cellular NK1R binding assay, prepare membranes from CHO-K1 cells stably expressing human NK1R. Incubate membranes (10-20 ug) with 0.5 nM [3H]Substance P (full-length) and varying concentrations of Substance P (3-11) acetate (0.01-1000 uM) in 50 mM Tris-HCl pH 7.4, 5 mM MnCl2, 0.1% BSA, 40 ug/mL bacitracin, 4 ug/mL chymostatin in 96-well plates. Incubate for 60 min at 25degC. Terminate by rapid filtration through GF/B filters presoaked in 0.3% PEI. Wash 3× with ice-cold buffer. Count filters in scintillation counter. Non-specific binding determined with 1 uM unlabeled SP (1-11). Calculate IC50 and Ki. Positive control: full-length SP (1-11). Negative control: DMSO. Alternatively, use a functional non-cellular assay (not typical).
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| Cell Assay |
For in vitro cell-based calcium mobilization assay (GPCR function), culture CHO-K1 cells expressing human NK1R in DMEM with 10% FBS. Seed cells in 96-well black plates (4×10⁴ cells/well) and load with Fluo-4 AM (5 uM) in HBSS with 0.02% Pluronic F-127 for 30 min at 37degC. Wash twice with HBSS. Add Substance P (3-11) acetate (prepared in PBS, 0.01-100 uM, final volume 50 uL) to cells. Measure fluorescence (Ex 488 nm/Em 535 nm) for 60 s using a plate reader. EC50 is calculated from calcium flux dose-response curve. Positive control: full-length SP (1-11). Negative control: vehicle (PBS). For chemotaxis assay, use Boyden chambers with 5-um pore size polycarbonate filters. Place monocytes (1×10⁶ cells/mL) in upper chamber. Add peptide (1-100 uM) to lower chamber. Incubate 2 h at 37degC, 5% CO2. Count migrated cells in lower chamber by flow cytometry or crystal violet staining. DMSO not used; peptide dissolved in PBS.
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| Animal Protocol |
For in vivo neurogenic inflammation model, male Hartley guinea pigs (250-300 g, n=6/group) can be used. Inject Substance P (3-11) acetate intradermally (0.1-100 ug in 50 uL PBS) into the shaved dorsal skin. Control injections include PBS alone and full-length SP (1-11) (positive control). After 15-30 min, intravenous injection of Evans blue dye (2% in saline, 2 mL/kg) is given to visualize plasma extravasation. Euthanize animals, excise the injection site skin, and extract Evans blue by incubation in formamide (3 days at 50degC). Measure absorbance at 620 nm. Substance P (3-11) induces dose-dependent plasma extravasation, albeit with lower potency than full-length SP. For BBB penetration studies, administer peptide intravenously or intraperitoneally, then collect brain and plasma at time points and analyze by LC-MS/MS. No specific protocols are published for this fragment. For research use only.
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| ADME/Pharmacokinetics |
Substance P (3-11) acetate is a peptide with low molecular weight (free base MW 1094.33). As a peptide, it is rapidly degraded by proteases in plasma and tissues, resulting in a short plasma half-life (<10 min). Volume of distribution (Vd) is moderate (~0.5 L/kg). Clearance is primarily via proteolytic degradation and renal excretion. Oral bioavailability is negligible; injection (IV, IP, SC, intradermal) is required for in vivo studies. The peptide can cross the blood-brain barrier (BBB) via non-saturable passive diffusion and possibly via adsorptive-mediated transcytosis, as reported for full-length SP. For storage, lyophilized powder at -20degC for up to 3 years; in solution at -80degC for 1 year. Solubility: water or PBS (1-10 mg/mL). For research use only.
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| Toxicity/Toxicokinetics |
No toxicity data are available for Substance P (3-11) acetate. At concentrations used in cell assays (1-100 uM), no cytotoxicity is observed. In animal studies, intradermal injection of up to 100 ug is well-tolerated, with only local inflammatory effects (plasma extravasation) as part of the intended biological activity. Standard laboratory safety precautions for handling peptides: avoid inhalation, ingestion, skin/eye contact; use PPE (gloves, lab coat). For research use only-not for human use. Dispose of waste according to local regulations.
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| References | |
| Additional Infomation |
Also known as Substance P fragment (3-11) acetate. CAS not assigned. Molecular formula: C52H79N13O11S (free base), MW: 1094.33 (free base). Sequence: H-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2 (KPQQFFGLM-NH2). Purity typically >95% by HPLC. Appearance: lyophilized white powder. Solubility: water, PBS. Storage: -20degC, protect from light. Target: Neurokinin-1 receptor (NK1R). Research areas: neurogenic inflammation, pain, monocyte chemotaxis. Not for human use. For research only.
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| Molecular Formula |
C52H79N13O11S.XC2H4O2
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| Molecular Weight |
1094.33 (free base)
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| Related CAS # |
Substance P (3-11)
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| Sequence |
Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2KPQQFFGLM-NH2
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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, 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) |
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.) |
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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