| 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 |
MC1R
MC1 receptor (Melanocortin 1 Receptor) |
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| ln Vitro |
ACTH.(1–17) Strong agonists of hMC1R include TFA. With a Ki value of 0.21±0.03 nM, the affinity of ACTH(1-17) for hMC1R is high, marginally higher than that of alpha-MSH at 0.13±0.005 nM[1]. Acth(1-17) stimulates growth hormone production in rat pituitary cultures even at micromolar doses [2], albeit not significantly.
As a potent agonist, ACTH (1-17) TFA exhibits high affinity for the human MC1 receptor with a Ki value of 0.21 nM, showing slightly higher affinity compared to alpha-MSH (Ki=0.13+/-0.005 nM). It also stimulates growth hormone production in rat pituitary cultures, though not significantly. |
| ln Vivo |
Two hours after the daily dark span begins, nocturnal animals become active, and inhibition of DNA tagging is observed when ACTH (1-17) is delivered. Larger doses in particular were linked to a 24-hour reduction of DNA labeling when given during this circadian phase. The inhibitory impact was significantly reduced when the same amount was administered four hours earlier [3].
In nocturnal animals, administration of ACTH (1-17) TFA during the dark phase inhibits DNA synthesis, with larger doses linked to a 24-hour reduction in DNA labeling. This inhibitory effect is significantly reduced when the compound is given at a different circadian time. |
| Enzyme Assay |
In a typical receptor binding assay, membrane preparations from cells expressing the human MC1 receptor are incubated with a labeled tracer (e.g., [125I]-NDP-alpha-MSH) in the presence of varying concentrations of the test compound in assay buffer (e.g., 50 mM Tris-HCl, pH 7.4, containing 0.2% BSA and 5 mM MgCl2). After incubation at room temperature for 60-90 minutes, the reaction is terminated by rapid filtration through GF/C filters, followed by washing. The retained radioactivity is then measured, and Ki values are calculated from competition curves.
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| Cell Assay |
For cell-based assays, cells endogenously expressing or transfected with the MC1 receptor (e.g., B16-F10 melanoma cells) are seeded in 96-well plates and grown to confluence. The cells are then treated with various concentrations of ACTH (1-17) TFA for a predetermined time (e.g., 30 min). After treatment, the cells are lysed, and the second messenger (e.g., cAMP) levels are measured using a specific ELISA or HTRF kit. EC50 values are then calculated from the dose-response curve.
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| Animal Protocol |
In a common protocol, male Sprague-Dawley rats are injected intracerebroventricularly with ACTH (1-17) TFA at various doses (e.g., 0.1-10 ug). After specified time points (e.g., 15, 30, 60, 120 minutes), the animals are sacrificed, and brain regions (e.g., hypothalamus, hippocampus) are dissected. Tissues are then processed for analysis of downstream signaling markers, such as phosphorylated ERK1/2, using Western blotting or ELISA.
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| ADME/Pharmacokinetics |
As a research-grade peptide, specific PK data for ACTH (1-17) TFA may be limited. However, as a polypeptide, it is generally expected to be rapidly degraded by proteases in the gastrointestinal tract and blood, leading to low oral bioavailability. Its in vivo half-life is typically short, often on the order of minutes. Administration is typically via injection (e.g., intravenous, intramuscular, or intraperitoneal).
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| Toxicity/Toxicokinetics |
Long-term toxicity and safety pharmacology studies have not been publicly reported for this research peptide. In vitro and in vivo studies suggest it can inhibit DNA synthesis, which may be a relevant effect for safety assessment. As with other peptides, potential toxicities are related to its pharmacological action of prolonged MC1 receptor activation, which could lead to issues like hyperpigmentation or adrenal hyperplasia.
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| References | |
| Additional Infomation |
The MC1 receptor is a key regulator of pigmentation and is also involved in anti-inflammatory responses and immunomodulation. ACTH (1-17) TFA is a synthetic corticotropin analog. Its parent hormone, ACTH, is used clinically as a diagnostic agent for adrenal insufficiency and as a therapeutic agent in conditions like infantile spasms. This peptide is for research use only and is not approved for clinical use.
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| Molecular Formula |
C95H145N29O23S.C2HF3O2
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|---|---|
| Molecular Weight |
2207.43
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| Related CAS # |
ACTH (1-17);7266-47-9
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| Appearance |
Solid powder
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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 :~100 mg/mL (~45.30 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (45.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4530 mL | 2.2651 mL | 4.5302 mL | |
| 5 mM | 0.0906 mL | 0.4530 mL | 0.9060 mL | |
| 10 mM | 0.0453 mL | 0.2265 mL | 0.4530 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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