| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
NK-2 receptor (tachykinin receptor 2). Neurokinin A is an activator of the NK-2 receptor and tachykinin receptors. It binds preferentially to the NK-2 receptor, which is a G protein-coupled receptor that activates phospholipase C and increases intracellular calcium. This binding mediates the contractile effects of Neurokinin A on smooth muscle in airways and gastrointestinal tissues.
|
|---|---|
| ln Vitro |
Neurokinin A (substance K) is a peptide neurotransmitter that belongs to the tachykinin family and may have a significant role in mediating interactions between human gastrointestinal and respiratory tissues. The NK-2 receptor, which is thought to be present on smooth muscle cells and pharmacologically linked to GTP-binding proteins, is how neurokinin A functions. A member of the peptide neurotransmitter family known as tachykinins is neurokinin A. These peptides have a wide tissue distribution and are connected to both the peripheral and central nervous systems. The COOH terminal structure of tachykinin is Phe-X-Gly-Leu-Met-NH. Substance P and neurokinin A or K are the most well-known members of this family [1].
Neurokinin A demonstrates potent contractile activity on smooth muscle in vitro, particularly in airway and gastrointestinal tissues. It has anti-proliferative effects on hematopoietic progenitor cells, which are partly mediated by p53 activating the 5' flanking region of the neurokinin-2 receptor. The compound acts as a peptide neurotransmitter and neuromodulator in various in vitro systems. |
| ln Vivo |
In vivo, Neurokinin A is a major mediator in human airway and gastrointestinal tissues. It has the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the bronchi. The compound is involved in the regulation of pain, inflammation, cardiovascular function, gastrointestinal motility, and immune response.
|
| Enzyme Assay |
In vitro receptor binding assays for Neurokinin A involve competition binding experiments using radiolabeled ligands such as [125I]-Neurokinin A. Membranes are prepared from cells expressing the NK-2 receptor. Neurokinin A is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves. Functional assays measure calcium mobilization or smooth muscle contraction.
|
| Cell Assay |
Cellular assays for Neurokinin A involve culturing cells expressing the NK-2 receptor, such as smooth muscle cells or transfected cell lines. Cells are treated with Neurokinin A at varying concentrations. Calcium mobilization is measured using fluorescent indicators. Smooth muscle contraction can be assessed using isolated tissue preparations. The compound's effects on cell proliferation can be evaluated using hematopoietic progenitor cell assays.
|
| Animal Protocol |
In vivo animal studies for Neurokinin A are typically conducted in rodent models to assess its effects on airway and gastrointestinal function. The compound is administered via intravenous or intraperitoneal injection. Bronchoconstriction, gastrointestinal motility, and cardiovascular parameters are measured. Dosing regimens vary depending on the study objectives.
|
| ADME/Pharmacokinetics |
Neurokinin A is a neuropeptide with a molecular weight of 1133.3 and a molecular formula of C50H80N14O14S. It is soluble in DMSO. The compound is typically supplied as a lyophilized solid and should be stored under recommended conditions. Detailed pharmacokinetic parameters are not extensively documented in publicly available sources.
|
| Toxicity/Toxicokinetics |
Neurokinin A is generally considered safe for research use at appropriate concentrations. Comprehensive toxicological data are limited. The compound is a naturally occurring neuropeptide and is not known to be highly toxic. It is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety precautions should be taken when handling the compound.
|
| References | |
| Additional Infomation |
mammalian neuropeptide composed of 10 amino acids, belonging to the tachykinin family. Its structure and function are similar to substance P and neurokinin B, capable of exciting neurons, dilating blood vessels, and contracting smooth muscle, such as the smooth muscle in the bronchi.
Neurokinin A (NKA) is a neuropeptide of the tachykinin family that acts as an activator of the NK-2 receptor. It is involved in pain, inflammation, cardiovascular function, gastrointestinal motility, and immune response. The compound is also known as Substance K and Neuromedin L. It is not approved for clinical use and is available for research purposes only. |
| Molecular Formula |
C50H80N14O14S
|
|---|---|
| Molecular Weight |
1133.3206
|
| Exact Mass |
1132.57
|
| CAS # |
86933-74-6
|
| Related CAS # |
Neurokinin A TFA;2828433-19-6
|
| PubChem CID |
5311311
|
| Appearance |
White to off-white solid powder
|
| Density |
1.305 g/cm3
|
| Boiling Point |
1610.7ºC at 760 mmHg
|
| Flash Point |
927.9ºC
|
| Index of Refraction |
1.58
|
| LogP |
1.053
|
| Hydrogen Bond Donor Count |
16
|
| Hydrogen Bond Acceptor Count |
18
|
| Rotatable Bond Count |
37
|
| Heavy Atom Count |
79
|
| Complexity |
2030
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC2=CN=CN2)N)O
|
| InChi Key |
HEAUFJZALFKPBA-JPQUDPSNSA-N
|
| InChi Code |
InChI=1S/C50H80N14O14S/c1-26(2)18-34(45(73)58-32(42(53)70)15-17-79-6)57-38(67)23-55-49(77)40(27(3)4)63-47(75)35(19-29-12-8-7-9-13-29)60-48(76)37(24-65)62-46(74)36(21-39(68)69)61-50(78)41(28(5)66)64-44(72)33(14-10-11-16-51)59-43(71)31(52)20-30-22-54-25-56-30/h7-9,12-13,22,25-28,31-37,40-41,65-66H,10-11,14-21,23-24,51-52H2,1-6H3,(H2,53,70)(H,54,56)(H,55,77)(H,57,67)(H,58,73)(H,59,71)(H,60,76)(H,61,78)(H,62,74)(H,63,75)(H,64,72)(H,68,69)/t28-,31+,32+,33+,34+,35+,36+,37+,40+,41+/m1/s1
|
| Chemical Name |
(3S)-3-[[(2S,3R)-2-[[(2S)-6-amino-2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]hexanoyl]amino]-3-hydroxybutanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-oxobutanoic acid
|
| 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 (In Vitro) |
H2O : ~100 mg/mL (~88.24 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
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 | 0.8824 mL | 4.4118 mL | 8.8236 mL | |
| 5 mM | 0.1765 mL | 0.8824 mL | 1.7647 mL | |
| 10 mM | 0.0882 mL | 0.4412 mL | 0.8824 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04468646 | Unknown status | Drug: NK-1R antagonist | Neurokinin 1 Receptor, Substance P, Respiratory Illness, Inflammation, Covid-19, Coronavirus | Prof. Dr. Fridoon Jawad Ahmad | 2020-06-15 | Phase 3 |
| NCT04676763 | Completed | Drug: Substance P Drug: Normal Saline Drug: Histamine |
Skin Diseases | GlaxoSmithKline | 2021-03-02 | Not Applicable |
| NCT06632080 | Not yet recruiting | Drug: Substance P Drug: Placebo |
Healthy Volunteers Only | Danish Headache Center | 2024-10-14 | Not Applicable |
| NCT01280149 | Completed | Biological: substance P Biological: substance P injections |
Seasonal Allergic Rhinitis | Northwestern University | 2011-01 | Phase 1 |
| NCT02820558 | Unknown status | Drug: Substance P | Diabetes Mellitus, Type 1 | Vanilloid Genetics Inc. | 2016-05 | Phase 1 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
