| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
ACTH (4-11) targets the melanocortin receptor 1 (MC1R), but with significantly reduced binding activity compared to full-length ACTH or α-MSH. MC1R is a G protein-coupled receptor that is primarily expressed on melanocytes and plays a key role in pigmentation and melanin synthesis. ACTH (4-11) is a fragment of adrenocorticotropin hormone that exhibits weak α-MSH potency only at high concentrations. This indicates that the N-terminal region of ACTH (residues 1-3) is critical for high-affinity binding and full agonist activity at MC1R.
|
|---|---|
| ln Vitro |
In vitro and in vivo differentiation of mouse epidermal melanocytes is induced by alpha-melanocyte-stimulating hormone (MSH). The amino acid sequence of MSH and adrenocorticotropic hormone (ACTH) is identical. α-MSH stimulates the in vitro and in vivo differentiation of mouse epidermal melanocytes. Nearly all of the activity of ACTH (4-11) binding to the melanocortin receptor 1 (MC1R) has been lost [1].
In vitro, ACTH (4-11) is an adrenocorticotropin hormone fragment that possesses weak α-melanocyte stimulating hormone (α-MSH) potency only at high doses (100 and 1000 nM). It loses almost all activity for binding to melanocortin receptor 1 (MC1R). This suggests that the fragment has significantly reduced receptor binding affinity and agonist activity compared to the full-length peptide. In cell-based assays, ACTH (4-11) can be used as a control peptide to study the structure-activity relationship of melanocortin peptides. |
| ln Vivo |
In vivo, ACTH (4-11) is used as a research peptide to study the structure-activity relationships of melanocortin peptides and their receptors. Its weak activity at MC1R makes it a useful tool for understanding the molecular determinants of receptor binding and activation. However, specific in vivo data for ACTH (4-11) are not detailed in the available literature. As a peptide fragment, it is not a therapeutic agent and is used primarily for research purposes.
|
| Enzyme Assay |
Non-cellular in vitro assays for ACTH (4-11) involve receptor binding studies. A standard protocol uses membrane preparations from cells expressing recombinant human melanocortin receptor 1 (MC1R). The membranes are incubated with a radiolabeled ligand, such as [¹²⁵I]NDP-α-MSH, and varying concentrations of ACTH (4-11). Non-specific binding is determined in the presence of an excess of unlabeled α-MSH. After incubation, the reaction is terminated by rapid filtration, and the radioactivity bound to the membranes is measured. The IC50 or Ki values are calculated from the competition curves.
|
| Cell Assay |
Cellular assays for ACTH (4-11) are performed using cell lines expressing MC1R, such as B16 melanoma cells. Cells are treated with ACTH (4-11) at various concentrations. The activation of MC1R is assessed by measuring intracellular cAMP accumulation using an ELISA or HTRF assay. The weak agonist activity of ACTH (4-11) is compared to that of full-length ACTH or α-MSH. The EC50 for cAMP accumulation is determined from the concentration-response curve.
|
| Animal Protocol |
In vivo animal studies for ACTH (4-11) are not common, as it is primarily a research peptide used in vitro. If used in vivo, it would be administered via injection to study its effects on melanocortin receptor signaling or pigmentation. However, due to its weak activity, it is unlikely to produce significant effects in vivo. Specific protocols are not available in the literature.
|
| ADME/Pharmacokinetics |
ACTH (4-11) has a molecular weight of 1090.26 and a CAS number of 67224-41-3. As a peptide, it has poor oral bioavailability and is typically administered via injection in research studies. It is stored as a powder at -20°C. Its solubility in water is limited but can be enhanced with mild acid or DMSO. Detailed pharmacokinetic parameters are not available, as it is not a drug candidate.
|
| Toxicity/Toxicokinetics |
ACTH (4-11) is a peptide fragment and is generally considered to have low toxicity. As a research peptide, it is not intended for human use and is strictly for preclinical research purposes. Standard safety precautions should be followed when handling ACTH (4-11). No specific toxicity data are available in the provided literature.
|
| References |
[1]. Hirobe T, et al. ACTH(4-12) is the minimal message sequence required to induce the differentiation of mouse epidermal melanocytes in serum-free primary culture. J Exp Zool. 2000 May 1;286(6):632-40.
|
| Additional Infomation |
ACTH (4-11) is an adrenocorticotropin hormone fragment (residues 4-11) that possesses weak α-MSH potency only at high doses (100 and 1000 nM). It loses almost all activity for binding to melanocortin receptor 1 (MC1R). The sequence is Met-Glu-His-Phe-Arg-Trp-Gly-Lys. ACTH (4-11) is used as a research peptide to study the structure-activity relationships of melanocortin peptides and their receptors. It is not a clinically approved drug and has not entered clinical trials. Its primary value is as a research tool for peptide biology and receptor pharmacology.
|
| Molecular Formula |
C50H71N15O11S
|
|---|---|
| Molecular Weight |
1090.27
|
| Exact Mass |
1089.52
|
| CAS # |
67224-41-3
|
| PubChem CID |
44134524
|
| Appearance |
White to off-white solid powder
|
| Density |
1.46 g/cm3
|
| Index of Refraction |
1.682
|
| LogP |
3.693
|
| Hydrogen Bond Donor Count |
15
|
| Hydrogen Bond Acceptor Count |
16
|
| Rotatable Bond Count |
35
|
| Heavy Atom Count |
77
|
| Complexity |
1980
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZKBNJKUZBFBIKV-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C50H71N15O11S/c1-77-21-18-33(52)43(69)61-36(16-17-42(67)68)46(72)65-40(24-31-26-55-28-59-31)48(74)63-38(22-29-10-3-2-4-11-29)47(73)62-35(15-9-20-56-50(53)54)45(71)64-39(23-30-25-57-34-13-6-5-12-32(30)34)44(70)58-27-41(66)60-37(49(75)76)14-7-8-19-51/h2-6,10-13,25-26,28,33,35-40,57H,7-9,14-24,27,51-52H2,1H3,(H,55,59)(H,58,70)(H,60,66)(H,61,69)(H,62,73)(H,63,74)(H,64,71)(H,65,72)(H,67,68)(H,75,76)(H4,53,54,56)
|
| Chemical Name |
6-amino-2-[[2-[[2-[[2-[[2-[[2-[[2-[(2-amino-4-methylsulfanylbutanoyl)amino]-4-carboxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-phenylpropanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]hexanoic acid
|
| Synonyms |
Acth (4-11) Acth 4-11 Corticotropin 4-11
|
| 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 (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)
|
| 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 | 0.9172 mL | 4.5860 mL | 9.1720 mL | |
| 5 mM | 0.1834 mL | 0.9172 mL | 1.8344 mL | |
| 10 mM | 0.0917 mL | 0.4586 mL | 0.9172 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 |
| NCT02446886 | TERMINATEDWITH RESULTS | Drug: Adrenocorticotropic hormone (ACTH) gel (H.P. Acthar®) | Multiple Sclerosis | Weill Medical College of Cornell University | 2016-06 | Phase 4 |
| NCT02132195 | COMPLETEDWITH RESULTS | Drug: ACTH | Nephrotic Syndrome | Emory University | 2014-05 | Phase 3 |
| NCT01769937 | COMPLETED | Drug: H.P. Acthar Gel | Lupus Erythematosus Systemic Exacerbation | Fiechtner, Justus J., M.D., P.C. | 2012-10 | Phase 4 |
| NCT02315872 | COMPLETEDWITH RESULTS | Drug: ACTH Drug: Placebo |
Multiple Sclerosis, Relapsing-Remitting | Providence Health & Services | 2015-05-22 | Phase 3 |
| NCT01093157 | COMPLETED | Drug: Adrenocorticotrophic hormone ACTH | Glomerulonephritis/td> | University Health Network, Toronto | 2010-02 | Phase 1 Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
