| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Kinetensin does not have a single well-defined target. It is a neurotensin-like peptide that increases vascular permeability and releases histamine from rat mast cells. It may function as an inflammatory mediator. Its activity is related to its role in modulating physiological processes, particularly in vascular and neurobiology.
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| ln Vitro |
When rat peritoneal mast cells are exposed to the peptide kinesin, which was extracted from human plasma treated with pepsin, it causes a dose-dependent release of histamine. The ideal concentration, which releases 80% of the total histamine, is between 100 and 1000 μM. The threshold concentration is roughly 1 μM, while the ED50 is 10 μM. Kinesin is comparable to the opioid peptide dynorphin and has a potency that is 10–100 times lower than neurotensin. Histamine releases at a temperature that is largely dependent on temperature; no release happens at 0 or 45 °C, and 37 °C is about the ideal. When extracellular calcium is not present, histamine release is greatly inhibited [2].
In vitro studies demonstrate that Kinetensin is a potent histamine releaser. It increases vascular permeability and is a neurotensin-like peptide. Its activity is assessed in assays measuring histamine release from mast cells. |
| ln Vivo |
Rats administered intradermally with dynamictensin also exhibit a dose-dependent increase in vascular permeability [2].
In vivo, Kinetensin is an endogenous peptide that may function as an inflammatory mediator. Its role in modulating vascular permeability and histamine release suggests it plays a part in inflammatory and allergic responses. |
| Enzyme Assay |
In vitro assays for Kinetensin involve measuring its ability to release histamine from mast cells. Rat mast cells are treated with the peptide, and the amount of histamine released into the supernatant is quantified. This assay is used to study its inflammatory activity.
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| Cell Assay |
Cellular assays for Kinetensin are not well-defined. Its effects can be studied in mast cell cultures, where histamine release is measured as a functional endpoint. It may also be studied in vascular endothelial cells to assess its effects on permeability.
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| Animal Protocol |
In vivo animal studies for Kinetensin are limited. For studying its role as an inflammatory mediator, animal models of inflammation could be used. The peptide could be administered, and its effects on vascular permeability and histamine release would be assessed.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Kinetensin are characteristic of a peptide. It has a molecular weight of 1172.38 and a molecular formula of C56H85N17O11. As a peptide, it has poor oral bioavailability and is rapidly degraded in vivo. It is typically stored at -20degC.
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| Toxicity/Toxicokinetics |
The toxicological data for Kinetensin are limited. As an endogenous peptide, it is not typically associated with toxicity at physiological levels. However, as an inflammatory mediator, its excessive release could contribute to pathological conditions.
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| References |
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| Additional Infomation |
Kinin is an oligopeptide composed of nine amino acids with the sequence L-Ile-L-Ala-L-Arg-L-Arg-L-His-L-Pro-L-Tyr-L-Phe-L-Leu. It was initially isolated from human plasma treated with pepsin and shares some sequence homology with the C-terminus of neurotensin. Kinin is a potent histamine releaser and may function as an inflammatory mediator. It is both a human metabolite and a histamine releaser. It is the binding base of kinin(2+).
Kinetensin is a neurotensin-like peptide isolated from human plasma. It is a member of the kinins family and is a biologically active fragment derived from kininogen. It increases vascular permeability and releases histamine, functioning as an inflammatory mediator. It is available for research use only. |
| Molecular Formula |
C56H85N17O11
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|---|---|
| Molecular Weight |
1172.3814
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| Exact Mass |
1171.66
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| CAS # |
103131-69-7
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| Related CAS # |
103131-69-7; Kinetensin TFA salt;
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| PubChem CID |
147043
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| Appearance |
White to off-white solid powder
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| Density |
1.41 g/cm3
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| Index of Refraction |
1.661
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| LogP |
4.334
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| Hydrogen Bond Donor Count |
15
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
34
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| Heavy Atom Count |
84
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| Complexity |
2240
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| Defined Atom Stereocenter Count |
10
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1=CN=CN1)C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](CC(C)C)C(=O)O)N
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| InChi Key |
PANUJGMSOSQAAY-IHXGQVBNSA-N
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| InChi Code |
InChI=1S/C56H85N17O11/c1-6-32(4)45(57)52(81)66-33(5)46(75)67-38(15-10-22-63-55(58)59)47(76)68-39(16-11-23-64-56(60)61)48(77)71-42(28-36-29-62-30-65-36)53(82)73-24-12-17-44(73)51(80)70-41(27-35-18-20-37(74)21-19-35)49(78)69-40(26-34-13-8-7-9-14-34)50(79)72-43(54(83)84)25-31(2)3/h7-9,13-14,18-21,29-33,38-45,74H,6,10-12,15-17,22-28,57H2,1-5H3,(H,62,65)(H,66,81)(H,67,75)(H,68,76)(H,69,78)(H,70,80)(H,71,77)(H,72,79)(H,83,84)(H4,58,59,63)(H4,60,61,64)/t32-,33-,38-,39-,40-,41-,42-,43-,44-,45-/m0/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-amino-3-methylpentanoyl]amino]propanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoic acid
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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) |
DMSO : ~100 mg/mL (~85.30 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8530 mL | 4.2648 mL | 8.5297 mL | |
| 5 mM | 0.1706 mL | 0.8530 mL | 1.7059 mL | |
| 10 mM | 0.0853 mL | 0.4265 mL | 0.8530 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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