| Size | Price | Stock | Qty |
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| Targets |
- Substance P 7-11 exerts biological effects on bovine articular chondrocytes [1]
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|---|---|
| ln Vitro |
PGE2 and collagenase synthesis are increased by substances (7–11) at concentrations higher than 1 μM. P Substance (7-11), but neither speed nor completeness of SP, SP-(1-4), SP-(1-6), SP-(8-11), or SP-(9-1 1) are affected. The intracellular calcium concentration is elevated as a result of the kinins NKA and NKB (the fluorescent dye Fura-2). Substance P(7-11) at 10 μM can alter intracellular calcium levels up to a maximum of 140±30 nM[1].
- In bovine articular chondrocyte cultures (stimulated with Substance P 7-11 at 10⁻⁸ M, 10⁻⁷ M, 10⁻⁶ M for 24 hours): Prostaglandin E2 (PGE2) production was measured by radioimmunoassay. Results showed dose-dependent increase in PGE2: 10⁻⁸ M induced a 2.1 ± 0.3-fold increase, 10⁻⁷ M a 3.5 ± 0.4-fold increase, and 10⁻⁶ M a 5.2 ± 0.5-fold increase compared to the control group [1] - In bovine articular chondrocytes loaded with the Ca²⁺-sensitive fluorescent probe fura-2/AM: Substance P 7-11 (10⁻⁷ M, 10⁻⁶ M) was added, and intracellular Ca²⁺ concentration ([Ca²⁺]i) was monitored by fluorescence spectroscopy. It caused a rapid (within 30 seconds) and concentration-dependent increase in [Ca²⁺]i: 10⁻⁷ M induced a peak [Ca²⁺]i of 320 ± 25 nM (vs. 80 ± 10 nM in control), and 10⁻⁶ M induced a peak of 580 ± 35 nM. The [Ca²⁺]i increase was partially blocked by removing extracellular Ca²⁺ (reduction by ~40%) [1] - In bovine articular chondrocytes treated with Substance P 7-11 (10⁻⁷ M, 10⁻⁶ M) for 48 hours: Collagenase (matrix metalloproteinase, MMP) activity in the culture supernatant was measured using [³H]-labeled type II collagen as substrate. It increased collagenase activity by 1.8 ± 0.2-fold (10⁻⁷ M) and 2.7 ± 0.3-fold (10⁻⁶ M) compared to the control group [1] |
| Cell Assay |
- Isolation and culture of bovine articular chondrocytes: Cartilage was harvested from the metacarpophalangeal joints of young calves, minced, and digested with collagenase and hyaluronidase for 16 hours at 37°C. Chondrocytes were isolated by centrifugation, resuspended in DMEM supplemented with 10% fetal bovine serum, and cultured at 37°C in 5% CO₂. Cells were used at passage 2–3 for experiments [1]
- PGE2 production assay: Chondrocytes were seeded in 24-well plates (5×10⁴ cells/well) and synchronized in serum-free DMEM for 24 hours. Substance P 7-11 (10⁻⁸ M–10⁻⁶ M) was added, and cells were incubated for another 24 hours. The supernatant was collected, and PGE2 concentration was measured by radioimmunoassay (using a specific antibody against PGE2 and [¹²⁵I]-labeled PGE2 tracer) [1] - Intracellular Ca²⁺ measurement: Chondrocytes were loaded with 5 μM fura-2/AM in HEPES-buffered saline (HBS) for 30 minutes at 37°C. After washing, Substance P 7-11 (10⁻⁷ M–10⁻⁶ M) was added to the HBS, and fluorescence intensity (excitation at 340 nm and 380 nm, emission at 510 nm) was recorded every 5 seconds. [Ca²⁺]i was calculated using the ratio of fluorescence intensities (F340/F380) [1] - Collagenase activity assay: Chondrocytes were seeded in 6-well plates (2×10⁵ cells/well) and treated with Substance P 7-11 (10⁻⁷ M–10⁻⁶ M) for 48 hours. The supernatant was mixed with [³H]-labeled type II collagen (substrate) and incubated at 37°C for 18 hours. The reaction was terminated by adding trichloroacetic acid, and the radioactivity of the soluble fraction (released by collagenase degradation) was measured by liquid scintillation counting [1] |
| References | |
| Additional Infomation |
L-Phe-L-Phe-Gly-L-Leu-L-Met-NH2 is a pentapeptide composed of L-phenylalanine, L-phenylalanine, glycine, L-leucine, and L-methionine amide linked by peptide bonds. It is the C-terminal fragment of substance P. Functionally, it is associated with L-leucine, L-methionine amide, L-phenylalanine, and glycine. It is the conjugate base of L-Phe-L-Phe-Gly-L-Leu-L-Met-NH2(1+). Substance P 7-11 is the C-terminal fragment of substance P (a neuropeptide), composed of the amino acid sequence Phe⁷-Phe⁸-Gly⁹-Leu¹⁰-Met¹¹. It retains some of the biological activity of the full-length substance P, but is more stable against enzymatic degradation [1]
- The mechanism by which substance P 7-11 regulates PGE2, intracellular Ca²⁺, and collagenase in chondrocytes is thought to involve the activation of G protein-coupled receptors (GPCRs) on the chondrocyte membrane. This activation triggers intracellular signaling pathways (e.g., the phospholipase C/inositol triphosphate pathway), mediating the release of Ca²⁺ from intracellular storage, and subsequently producing downstream effects on the production of inflammatory mediators and enzymes [1] - Substance P 7-11 may be involved in the pathogenesis of degenerative joint diseases (e.g., osteoarthritis) because it induces the production of PGE2 (a pro-inflammatory mediator) and collagenase (a matrix-degrading enzyme), which may lead to cartilage inflammation and degeneration [1] |
| Molecular Formula |
C31H44N6O5S
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|---|---|
| Molecular Weight |
612.78326
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| Exact Mass |
612.309
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| CAS # |
51165-05-0
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| PubChem CID |
3084967
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| Appearance |
White to off-white solid powder
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| Density |
1.207g/cm3
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| Boiling Point |
1003.3ºC at 760 mmHg
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| Flash Point |
560.6ºC
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| Index of Refraction |
1.577
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| LogP |
3.618
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
43
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| Complexity |
907
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)CNC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC2=CC=CC=C2)N
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| InChi Key |
RBKYMAQIAMFDOE-CQJMVLFOSA-N
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| InChi Code |
InChI=1S/C31H44N6O5S/c1-20(2)16-25(31(42)36-24(28(33)39)14-15-43-3)35-27(38)19-34-30(41)26(18-22-12-8-5-9-13-22)37-29(40)23(32)17-21-10-6-4-7-11-21/h4-13,20,23-26H,14-19,32H2,1-3H3,(H2,33,39)(H,34,41)(H,35,38)(H,36,42)(H,37,40)/t23-,24-,25-,26-/m0/s1
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| Chemical Name |
(2S)-N-[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]-2-[[2-[[(2S)-2-[[(2S)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-4-methylpentanamide
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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) |
H2O : ~1.96 mg/mL (~3.20 mM)
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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 | 1.6319 mL | 8.1595 mL | 16.3191 mL | |
| 5 mM | 0.3264 mL | 1.6319 mL | 3.2638 mL | |
| 10 mM | 0.1632 mL | 0.8160 mL | 1.6319 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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