| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
alpha-MSH (11-13) acetate targets the melanocortin receptor pathway, specifically via activation of melanocortin receptors (MC1R, MC3R, MC4R, MC5R) but with lower affinity and different selectivity compared to full-length alpha-MSH. The KPV tripeptide is the minimal C-terminal sequence required for anti-inflammatory and antipyretic activity, while the N-terminal region of alpha-MSH (including the His-Phe-Arg-Trp sequence) is required for melanotropic activity. Thus, alpha-MSH (11-13) is devoid of pigmentary effects but retains the ability to suppress fever and inflammation. It operates within the melanocortin receptor and anti-inflammatory pathways. The exact receptor selectivity for KPV is not fully characterized but likely involves MC1R and/or MC3R.
|
|---|---|
| ln Vitro |
In vitro, alpha-MSH (11-13) acetate exhibits anti-inflammatory activity but no melanotropic activity. It inhibits the production of pro-inflammatory cytokines (e.g., IL-1beta, TNF-alpha, IL-6) in activated immune cells (e.g., macrophages, microglia) at concentrations of 0.1-100 uM. It also reduces nitric oxide (NO) production in LPS-stimulated macrophages. The tripeptide does not stimulate melanogenesis in B16 melanoma cells, in contrast to full-length alpha-MSH, confirming lack of melanotropic activity. No cytotoxicity is observed at effective concentrations. The peptide is dissolved in water or PBS; DMSO is not typically used. Positive control: alpha-MSH (1-13) full-length for anti-inflammatory activity, or for melanogenesis, alpha-MSH is the positive control. Negative control: vehicle.
|
| ln Vivo |
In vivo, alpha-MSH (11-13) acetate reduces fever in rabbits. In a standard antipyretic assay, rabbits are injected with bacterial lipopolysaccharide (LPS) or interleukin-1 (IL-1) intravenously to induce fever (increase in body temperature). Administration of alpha-MSH (11-13) acetate (10-100 ug/kg, intravenous or intracerebroventricular) significantly attenuates the fever response, as measured by rectal temperature over 2-4 h. The antipyretic effect is dose-dependent. The peptide also has anti-inflammatory effects in models of inflammation (e.g., carrageenan-induced paw edema) and protects against endotoxic shock. For research use only.
|
| Enzyme Assay |
Not applicable. alpha-MSH (11-13) acetate is a tripeptide that exerts its anti-inflammatory and antipyretic effects via activation of melanocortin receptors, which are G protein-coupled receptors (GPCRs) expressed on immune cells and in the hypothalamus. Its activity requires cell-based signaling. Non-cellular (acellular) binding assays to purified melanocortin receptors can be performed using membrane preparations, but the protocol is cell-based (though not using intact, living cells). For a truly acellular assay, one could use purified receptor in nanodiscs with radioligand binding, but such protocols are not standard. The primary characterization is through in vitro cell assays (cytokine inhibition) and in vivo rabbit fever models. No enzyme inhibition assays are performed.
|
| Cell Assay |
For in vitro anti-inflammatory assays, culture RAW264.7 mouse macrophages in DMEM with 10% FBS at 37degC, 5% CO2. Seed cells in 96-well plates (1×10⁵ cells/well). After 24 h, pre-treat with alpha-MSH (11-13) acetate at 0.1, 1, 10, 50, 100 uM (from 10 mM stock in PBS or water) for 1 h. Then add LPS (100 ng/mL) to stimulate inflammation. Incubate for 24 h. Collect supernatant for cytokine measurement (IL-1beta, TNF-alpha, IL-6) by ELISA. For NO measurement, add 100 uL of culture supernatant to 100 uL of Griess reagent (0.1% N-1-naphthylethylenediamine dihydrochloride, 1% sulfanilamide in 5% phosphoric acid) and read absorbance at 540 nm. For cell viability, use MTT assay. Positive control: full-length alpha-MSH (1-13) (1-10 uM) for anti-inflammatory effects. Negative control: vehicle (PBS). All experiments in triplicate. DMSO not used. For B16 melanoma melanogenesis assay, culture B16-F10 cells in DMEM with 10% FBS. Treat with alpha-MSH (11-13) (0.1-100 uM) for 72 h. Positive control: alpha-MSH (1-13) (100 nM). Measure melanin content as absorbance at 405 nm. alpha-MSH (11-13) should not increase melanin.
|
| Animal Protocol |
For in vivo rabbit fever model, use male New Zealand White rabbits (2-3 kg, n=6/group). Measure baseline rectal temperature using a digital thermometer inserted 10 cm into the rectum. Inject LPS from E. coli (0.1-1 ug/kg) intravenously via ear vein to induce fever. Administer alpha-MSH (11-13) acetate (10, 30, 100 ug/kg) intravenously (IV) or intracerebroventricularly (ICV) simultaneously with LPS or 30 min prior. Control groups: vehicle (sterile saline), LPS alone, alpha-MSH alone. Record rectal temperature every 30 min for 4 h post-LPS. Data expressed as change in body temperature (deltadegC) from baseline. alpha-MSH (11-13) (30-100 ug/kg IV) significantly reduces the fever response by 0.5-1.0degC compared to LPS alone. For endotoxic shock model, inject rabbits with LPS (10 ug/kg IV) and co-administer alpha-MSH (11-13) (100-500 ug/kg). Monitor survival over 48 h. The peptide improves survival and reduces hypotension. No significant toxicity observed. For research use only.
|
| ADME/Pharmacokinetics |
alpha-MSH (11-13) acetate is a small tripeptide (MW 402.49 as acetate salt, 386.49 as free base). As a tripeptide, it is rapidly degraded by plasma and tissue proteases, resulting in a short plasma half-life (<10-30 min). Volume of distribution (Vd) is moderate (~0.3-0.5 L/kg). Clearance is primarily renal and proteolytic. Oral bioavailability is negligible; injection (IV, IP, ICV) is required for in vivo studies. The peptide crosses the blood-brain barrier to some extent, enabling central antipyretic effects. For storage, lyophilized powder at -20degC for up to 3 years; in solution at -80degC for 6 months. Solubility: water or PBS. For research use only.
|
| Toxicity/Toxicokinetics |
No formal toxicity data are available for alpha-MSH (11-13) acetate. In rabbit studies, doses up to 500 ug/kg IV are well-tolerated without observable adverse effects (e.g., no change in heart rate, respiratory rate, or behavior). As a fragment of an endogenous peptide, it is expected to be of low toxicity. Standard laboratory safety precautions for handling peptides: avoid inhalation, ingestion, skin/eye contact; use PPE (gloves, lab coat). For research use only-not for human use. Dispose of waste according to local regulations.
|
| References | |
| Additional Infomation |
Also known as KPV acetate, ACTH-(11-13) acetate, Lys-Pro-Val acetate. CAS: 2828433-34-5. Molecular formula: C18H34N4O6, molecular weight: 402.49 (acetate salt). Sequence: Lys-Pro-Val (KPV). Purity: 99.3% by HPLC. Appearance: white to off-white solid powder. Solubility: water (freely soluble), DMSO, ethanol. Storage: -20degC powder for 3 years, 4degC for 2 years; in solution -80degC for 6 months. Target: melanocortin receptors (presumed MC1R/MC3R). Research areas: inflammation, fever, immunomodulation. Not for human use. For research only.
|
| Molecular Formula |
C18H34N4O6
|
|---|---|
| Molecular Weight |
402.49
|
| CAS # |
2828433-34-5
|
| Related CAS # |
α-MSH (11-13)
|
| Sequence |
Lys-Pro-ValKPV
|
| Appearance |
White to off-white solid powder
|
| Synonyms |
ACTH-(11-13) acetate; Lys-Pro-Val acetate; H-Lys-Pro-Val-OH acetate
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.4845 mL | 12.4227 mL | 24.8453 mL | |
| 5 mM | 0.4969 mL | 2.4845 mL | 4.9691 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4845 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
