| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary target of Hemokinin 1 (mouse) is the neurokinin-1 (NK1) receptor, a G protein-coupled receptor that is the primary mediator of substance P signaling. The peptide acts as a high-affinity and selective agonist at the NK1 receptor with a Ki of 0.175 nM. It shows significantly lower affinity for the NK2 receptor (Ki = 560 nM), demonstrating its selectivity for NK1. The NK1 receptor is involved in pain transmission, inflammation, smooth muscle contraction, and various neurogenic processes. Hemokinin 1 is also involved in acute airway inflammation in the mouse.
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| ln Vitro |
Concentration-dependent RUB contractions averaging 66±3% (n=6) of the maximal contraction induced by KCl (80 mM) were produced by hemokinin 1 (mouse) (1 nM-3 μM). Both neurokinin B (NKB) and the tachykinin NK3 receptor selective agonist Senktide cause a rapidly developing contractile response to GPI, as does hemokinin 1 (mouse) (10 nM–10 μM). Although it is 500 times less potent than NKB, mouse hemokinin 1 (H1) still causes a complete agonist response [1].
In vitro studies have demonstrated that Hemokinin 1 (mouse) is a potent and selective agonist at the NK1 receptor. It exhibits a Ki of 0.175 nM for the human NK1 receptor and shows approximately 3,200-fold selectivity over the NK2 receptor (Ki = 560 nM). The peptide induces full agonist responses in functional assays, though with approximately 500-fold lower potency compared to neurokinin B (NKB). These in vitro characteristics make Hemokinin 1 a valuable tool for studying NK1 receptor signaling and its role in various physiological and pathological processes, including inflammation and pain. |
| ln Vivo |
Dose-related hypotension is induced by mouse hemokinin 1 (0.01-100 nmol/kg iv, n = 10), with a maximal dose of 10 nmol/kg. The ED50 value of kinin 1 (mouse) for systolic blood pressure (SBP) is 0.2 nmol/kg (0.1-0.4 nmol/kg). The ED50 of mouse kinin 1 for diastolic blood pressure (DBP) is 0.1 nmol/kg (0.07-0.2 nmol/kg). In rats given atropine beforehand, hemokinin 1 (mouse) (0.1-100 nmol/kg) promotes dose-related salivation [1].
In vivo studies of Hemokinin 1 (mouse) have focused on its role in acute airway inflammation in the mouse model. As a selective NK1 receptor agonist, the peptide can be used to investigate the physiological and pathological roles of NK1 receptor activation in vivo. Its involvement in airway inflammation suggests that Hemokinin 1 may play a role in respiratory diseases and inflammatory conditions. The peptide's high affinity and selectivity for the NK1 receptor make it a useful tool for studying the consequences of NK1 activation in various tissues and disease models. Further in vivo studies may elucidate additional physiological functions of this endogenous peptide. |
| Enzyme Assay |
For in vitro enzyme/receptor binding assays, Hemokinin 1 (mouse) can be evaluated using radioligand binding studies with membranes expressing the human NK1 or NK2 receptors. Competition binding experiments using a labeled NK1 receptor antagonist (such as [3H]-substance P or a related radioligand) can determine the peptide's affinity (Ki) for the receptor. Saturation binding assays may be performed to characterize the binding kinetics. Functional assays such as calcium mobilization, IP1 accumulation, or cAMP inhibition can be used to assess agonist activity. Dose-response curves are generated to determine EC₅0 values and intrinsic activity. Standard assay conditions include physiological buffer systems with appropriate protease inhibitors to prevent peptide degradation.
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| Cell Assay |
For in vitro cellular experiments, Hemokinin 1 (mouse) is typically tested in cell lines expressing the human NK1 receptor, such as CHO or HEK293 cells stably transfected with the receptor, or in neuroblastoma cell lines that endogenously express NK1. Cells are cultured in appropriate media and treated with various concentrations of the peptide (typically ranging from picomolar to micromolar). Receptor activation is measured using calcium-sensitive dyes, IP1 accumulation assays, or cAMP inhibition assays. Signaling pathway activation can be further investigated using phospho-protein analysis or gene expression profiling. The peptide's stability in cell culture medium should be monitored, as peptidases may degrade Hemokinin 1 over time.
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| Animal Protocol |
For in vivo animal experiments, Hemokinin 1 (mouse) can be administered to rodents via various routes including intravenous injection, intraperitoneal injection, or intrathecal administration for studies of pain and inflammation. The peptide's involvement in acute airway inflammation can be studied in mouse models of airway inflammation. Typical doses may range from microgram to milligram quantities depending on the study objectives. Physiological parameters such as airway resistance, inflammatory cell infiltration, and cytokine levels can be measured. Behavioral assays for pain and nociception may be used to assess NK1-mediated effects. Animal studies should follow appropriate ethical guidelines and use suitable control groups for comparison.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Hemokinin 1 (mouse) have not been extensively characterized in the literature. As a peptide, it is expected to have very low oral bioavailability due to degradation in the gastrointestinal tract. When administered systemically, Hemokinin 1 would likely be rapidly cleared from circulation by peptidases and proteases. The half-life in plasma is expected to be short, typical of endogenous peptide hormones. Its distribution would be influenced by its size (1413.65 g/mol) and hydrophilic nature. The peptide would be metabolized to its constituent amino acids. Further pharmacokinetic studies would be needed to fully characterize its absorption, distribution, metabolism, and excretion profile in vivo.
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| Toxicity/Toxicokinetics |
Toxicological data for Hemokinin 1 (mouse) are limited, as the peptide is primarily a research tool for studying NK1 receptor biology. As an endogenous peptide, it is generally considered to have low toxicity at physiological concentrations. However, pharmacological doses could potentially lead to excessive NK1 receptor activation and associated effects such as hypotension, bronchoconstriction, or neurogenic inflammation. Standard toxicological assessments would include acute toxicity studies, repeated-dose toxicity studies, and evaluation of potential immunogenicity (for peptide therapeutics). As a research peptide, appropriate safety precautions should be taken when handling Hemokinin 1, including the use of personal protective equipment and proper laboratory practices.
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| References | |
| Additional Infomation |
Hemokinin 1 (mouse) is a research peptide used to study tachykinin NK1 receptor biology. No clinical trials or regulatory approvals have been reported for this peptide as a therapeutic agent. It is available from various peptide suppliers for research purposes only. The peptide's high affinity and selectivity for the NK1 receptor (Ki = 0.175 nM for NK1 vs. 560 nM for NK2) make it a valuable tool for studying NK1-mediated signaling and physiology. Its involvement in acute airway inflammation highlights its potential relevance to inflammatory diseases. Hemokinin 1 serves as a useful probe for investigating the role of the NK1 receptor in pain, inflammation, and other neurogenic processes.
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| Molecular Formula |
C61H100N22O15S
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|---|---|
| Molecular Weight |
1413.6501
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| Exact Mass |
1412.75
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| CAS # |
208041-90-1
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| PubChem CID |
90479800
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| Appearance |
White to off-white solid powder
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| Density |
1.483 g/cm3
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| LogP |
2.279
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
47
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| Heavy Atom Count |
99
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| Complexity |
2720
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| Defined Atom Stereocenter Count |
11
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)N)O
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| InChi Key |
ZOLDEMZLDJFVRY-RULPZMNSSA-N
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| InChi Code |
InChI=1S/C61H100N22O15S/c1-32(2)27-42(55(95)76-38(49(64)89)22-26-99-4)75-47(88)30-74-51(91)43(29-35-16-18-36(86)19-17-35)80-56(96)44(28-34-11-6-5-7-12-34)81-53(93)41(20-21-46(63)87)78-52(92)39(14-9-24-72-60(67)68)79-58(98)48(33(3)85)83-54(94)40(15-10-25-73-61(69)70)77-57(97)45(31-84)82-50(90)37(62)13-8-23-71-59(65)66/h5-7,11-12,16-19,32-33,37-45,48,84-86H,8-10,13-15,20-31,62H2,1-4H3,(H2,63,87)(H2,64,89)(H,74,91)(H,75,88)(H,76,95)(H,77,97)(H,78,92)(H,79,98)(H,80,96)(H,81,93)(H,82,90)(H,83,94)(H4,65,66,71)(H4,67,68,72)(H4,69,70,73)/t33-,37+,38+,39+,40+,41+,42+,43+,44+,45+,48+/m1/s1
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| Chemical Name |
(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxypropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-hydroxybutanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-N-[(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-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]pentanediamide
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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. |
| 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 (~70.74 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 | 0.7074 mL | 3.5369 mL | 7.0739 mL | |
| 5 mM | 0.1415 mL | 0.7074 mL | 1.4148 mL | |
| 10 mM | 0.0707 mL | 0.3537 mL | 0.7074 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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