2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Spantide I

Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.

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Custom Peptide Synthesis

Spantide I Chemical Structure

Spantide I Chemical Structure

CAS No. : 91224-37-2

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Based on 1 publication(s) in Google Scholar

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Description

Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation[1][2][3].

IC50 & Target[2]

NK1

230 nM (Ki)

NK2

8150 nM (Ki)

In Vivo

Spantide I (50 and 100 nM perfused through the cerebral ventricles) causes a complete respiratory arrest in all of the examined animals[2].
Spantide I (36 μg/mouse, ip daily) significantly decreases the number of perforated corneas, bacterial counts, and PMNs. Spantide I also downregulates the mRNA levels for type I cytokines (e.g., IFN-γ) as well as MIP-2, IL-6, TNF-α, and IL-1β[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female, 8-week-old C57BL/6 (B6) and BALB/c mice[3].
Dosage: 36 μg/mouse.
Administration: IP on days -1 and 0 (day of infection) and daily through 5 days pi (post infection).
Result: At 3 and 5 days pi, compound-treated mice had significantly less severe ocular disease than did the PBS-treated mice.
Contained significantly fewer PMNs than the corneas of PBS-treated mice at 3 and 5 days pi.
Significantly reduced levels of corneal TNF-α mRNA at 3 and 5 days pi.
Significantly reduced the level of IL-18 mRNA at 1 day pi.
Molecular Weight

1497.79

Formula

C75H108N20O13
CAS No.
Appearance

Solid

Color

White to off-white

Sequence Shortening

{D-Arg}-PKPQQ-{D-Trp}-F-{D-Trp}-LL-NH2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (66.77 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6677 mL 3.3383 mL 6.6765 mL
5 mM 0.1335 mL 0.6677 mL 1.3353 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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V1

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.6677 mL 3.3383 mL 6.6765 mL 16.6913 mL
5 mM 0.1335 mL 0.6677 mL 1.3353 mL 3.3383 mL
10 mM 0.0668 mL 0.3338 mL 0.6677 mL 1.6691 mL
15 mM 0.0445 mL 0.2226 mL 0.4451 mL 1.1128 mL
20 mM 0.0334 mL 0.1669 mL 0.3338 mL 0.8346 mL
25 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.6677 mL
30 mM 0.0223 mL 0.1113 mL 0.2226 mL 0.5564 mL
40 mM 0.0167 mL 0.0835 mL 0.1669 mL 0.4173 mL
50 mM 0.0134 mL 0.0668 mL 0.1335 mL 0.3338 mL
60 mM 0.0111 mL 0.0556 mL 0.1113 mL 0.2782 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Spantide I Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Spantide I91224-37-2Neurokinin ReceptorNK receptorTachykinin receptorIL-10TNF-αIL-18IFN-γPMNMIP-2IL-6IL-1βInhibitorinhibitorinhibit

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