Spantide

Alias: Substance P, arg(1)-trp(7,9)-leu(11)-; Spantide I; Spantide
Cat No.:V15093 Purity: ≥98%
Spantide I is an analog of substance P and a selective neurokinin-1 receptor (NK1 receptor) antagonist.
Spantide Chemical Structure CAS No.: 91224-37-2
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
Spantide I is an analog of substance P and a selective neurokinin-1 receptor (NK1 receptor) antagonist. Its Kis for NK1 and NK2 receptors are 230 nM and 8150 nM respectively. Spantide I significantly reduces corneal perforation by reducing type 1 cytokines and enhancing type 2 cytokine IL-10 in infected cornea.
Biological Activity I Assay Protocols (From Reference)
ln Vivo
In every animal studied, intrathecal infusion of spatide I at concentrations of 50 and 100 nM resulted in total respiratory arrest [2]. The number of perforated corneas, bacterial counts, and PMNs were all considerably decreased by spatide I (36 μg/mouse, intraperitoneal injection, every day). Spantide I also reduces the amounts of type I cytokines' mRNA, including MIP-2, IL-6, TNF-α, and IL-1β, as well as IFN-γ [3].
Animal Protocol
Animal/Disease Models: female, 8weeks old C57BL/6 (B6) and balb/c (Bagg ALBino) mouse [3].
Doses: 36 micrograms/mouse.
Route of Administration: IP on days -1 and 0 (day of infection) and one time/day for 5 days post-infection (post-infection).
Experimental Results: On days 3 and 5 post-injection, the severity of ocular disease in mice treated with compound was Dramatically less than that in mice treated with PBS. On days 3 and 5 after inoculation, PMN content was Dramatically diminished compared with PBS-treated mouse cornea. Corneal TNF-α mRNA levels were Dramatically diminished on the 3rd and 5th postoperative days. IL-18 mRNA levels were Dramatically diminished on day 1 after injection.
References
[1]. J C Beaujouan, et al. Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists. Br J Pharmacol. 1993 Mar;108(3):793-800.
[2]. M Zubrzycka, et al. Comparison of antagonistic properties of substance P analogs, spantide I, II and III, on evoked tongue jerks in rats. Endocr Regul. 2000 Mar;34(1):13-8.
[3]. Linda D Hazlett, et al. Spantide I decreases type I cytokines, enhances IL-10, and reduces corneal perforation in susceptible mice after Pseudomonas aeruginosa infection. Invest Ophthalmol Vis Sci. 2007 Feb;48(2):797-807.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C75H108N20O13
Molecular Weight
1497.81
Exact Mass
1496.8405
CAS #
91224-37-2
Related CAS #
Spantide I TFA
SMILES
CC(C[C@H](NC([C@@H](NC([C@H](NC([C@@H](NC([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=CNC4=CC=CC=C34)=O)CC5=CC=CC=C5)=O)CC6=CNC7=CC=CC=C67)=O)CC(C)C)=O)C(N)=O)C
Synonyms
Substance P, arg(1)-trp(7,9)-leu(11)-; Spantide I; Spantide
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
H2O : ~100 mg/mL (~66.77 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.6676 mL 3.3382 mL 6.6764 mL
5 mM 0.1335 mL 0.6676 mL 1.3353 mL
10 mM 0.0668 mL 0.3338 mL 0.6676 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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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