| 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 |
Neurokinin-1 receptor (NK1 receptor). Spantide I TFA is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for the NK1 and NK2 receptors, respectively. By blocking the NK1 receptor, it inhibits the binding of the endogenous ligand, substance P, thereby suppressing downstream signaling involved in pain, inflammation, and smooth muscle contraction.
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| ln Vitro |
In vitro, Spantide I TFA selectively antagonizes NK1 receptors, effectively blocking substance P-induced signaling. It is used to dissect the role of substance P in cellular models, including mast cell degranulation, cytokine production, and neuronal activation. By inhibiting the NK1 receptor, Spantide I demonstrates anti-inflammatory properties, such as reducing the production of type I cytokines like IFN-gamma.
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| ln Vivo |
In every animal studied, pantide I (perfused at 50 and 100 nM through the cerebral ventricles) results in total respiratory arrest[2]. Spantide I (36 μg/mouse, i.p. daily) dramatically reduces the quantity of microorganisms, PMNs, and perforated corneas. Spantide I also decreases the amounts of MIP-2, IL-6, TNF-α, IL-1β, and type I cytokines (e.g., IFN-γ) in the mRNA[3].
In vivo, Spantide I TFA exhibits significant anti-inflammatory activity. In a mouse model of Pseudomonas aeruginosa keratitis, daily intraperitoneal injection of Spantide I (36 microg/mouse) dramatically reduced corneal perforation, PMN infiltration, and the levels of inflammatory mediators MIP-2, IL-6, TNF-alpha, and IL-1beta. Intracerebroventricular (i.c.v.) administration of 50-100 nM has been shown to induce total respiratory arrest in animal studies. |
| Enzyme Assay |
Non-cell-based binding assays are used to confirm receptor selectivity. Membranes from CHO cells expressing the human NK1 receptor are incubated with [3H]Substance P (0.5 nM) and increasing concentrations of Spantide I TFA (0-1000 nM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MnCl2, 0.1% BSA) for 60 min. Non-specific binding is determined with 10 uM unlabeled Substance P. Bound radioactivity is separated by filtration, and Ki values are calculated.
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| Cell Assay |
A cellular NK1 receptor functional assay (e.g., Ca2+ flux) is performed. NK1R-expressing cells (e.g., CHO-NK1R or U373 MG cells) are loaded with a calcium-sensitive fluorescent dye. Cells are pre-treated with Spantide I TFA (0-1000 nM) for 15 min and then stimulated with 1-10 nM Substance P. The change in intracellular calcium is measured using a fluorescence plate reader. The IC50 for antagonism is determined.
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| Animal Protocol |
Animal/Disease Models: Female, 8 weeks old C57BL/6 (B6) and balb/c (Bagg ALBino) mouse[3].
Doses: 36 μg/mouse. Route of Administration: IP on days -1 and 0 (day of infection) and daily through 5 days pi (post infection) . Experimental Results: At 3 and 5 days pi, compound-treated mice had Dramatically less severe ocular disease than did the PBS-treated mice. Contained Dramatically fewer PMNs than the corneas of PBS-treated mice at 3 and 5 days pi. Dramatically decreased levels of corneal TNF-α mRNA at 3 and 5 days pi. Dramatically decreased the level of IL-18 mRNA at 1 day pi. Keratitis model: Female C57BL/6 mice receive a corneal scratch and are topically infected with P. aeruginosa. Spantide I TFA (36 microg/mouse) is administered via intraperitoneal injection on days -1 and 0 (day of infection), and then daily through day 5 post-infection. Eyes are examined daily by slit-lamp biomicroscopy for the development of corneal perforation. At the study endpoint, corneas are excised for histological analysis and assessment of inflammatory cytokines. |
| ADME/Pharmacokinetics |
Detailed PK data for Spantide I TFA is limited. As a peptide (MW ~1545), it has a short plasma half-life due to rapid proteolytic degradation, typically on the order of minutes. It is usually administered via intraperitoneal, intravenous, or subcutaneous injection, as it has poor oral bioavailability. The TFA salt form enhances solubility in aqueous buffers.
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| Toxicity/Toxicokinetics |
Spantide I TFA is intended for research use only and is not approved for human use. In animal studies, at the effective intraperitoneal dose of 36 microg/mouse, no gross acute toxicity was reported. However, central administration at higher doses (i.c.v.) can induce severe effects like respiratory arrest, indicating a high potential for central nervous system toxicity. Users should avoid self-administration.
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| References |
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| Additional Infomation |
Spantide I TFA is a research chemical and not a drug candidate. It is a valuable tool for studying the role of substance P and NK1 receptors in pain, inflammation, and cancer. The TFA salt form is stable, and the powder should be stored at -20degC. The compound is not for clinical use and should be handled with appropriate safety equipment.
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| Molecular Formula |
C75H108N20O13.XC2HF3O2
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| Related CAS # |
Spantide I;91224-37-2
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| Appearance |
White to off-white 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) |
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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