![[Ala17]-MCH](/upload/1124/V70558.png)
| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Ki: 0.16 nM (MCHR1) Ki: 34 nM (MCHR2)[1]
MCH1 and MCH2 (melanin-concentrating hormone) receptors. [Ala17]-MCH is a potent agonist at both receptor subtypes. |
|---|---|
| ln Vitro |
[Ala17]-MCH is a potent MCH receptor agonist with Ki values of 0.16 nM for MCH1 and 34 nM for MCH2. It displays selectivity for MCH1 over MCH2 (Ki ratio ~212-fold). In functional assays, it exhibits EC50 values of 17 nM at MCH1 and 54 nM at MCH2 receptors. The Eu3+-chelated labeled form shows high affinity for MCH1 (Kd = 0.37 nM) and low affinity for MCH2.
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| ln Vivo |
No detailed in vivo activity data are publicly available for [Ala17]-MCH. As a potent MCH receptor agonist, its in vivo effects would be expected to be related to the physiological roles of MCH receptors, including regulation of feeding behavior, energy homeostasis, and stress responses.
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| Enzyme Assay |
In vitro receptor binding assays are performed to determine the affinity of [Ala17]-MCH for MCH1 and MCH2 receptors. Radioligand binding studies using membrane preparations from cells expressing the receptors are conducted. The compound's ability to displace a specific radiolabeled ligand from each receptor is measured to calculate its Ki values. The Eu3+-chelated labeled form is used in binding studies to assess receptor affinity.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing recombinant MCH1 or MCH2 receptors. The cells are treated with [Ala17]-MCH, and receptor activation is measured by assessing downstream signaling events such as calcium mobilization or inhibition of cAMP accumulation. The EC50 values for the agonistic effect are determined from the concentration-response curves.
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| Animal Protocol |
In vivo studies would be conducted in animal models to evaluate the effects of [Ala17]-MCH on feeding behavior, energy homeostasis, and stress responses. The compound's effects on food intake, body weight, and anxiety-like behavior could be assessed in appropriate models.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for [Ala17]-MCH. As a peptide, its pharmacokinetic properties would be characterized by limited oral bioavailability and rapid clearance. Its ADME properties would be studied in preclinical models to guide in vivo experiments.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for [Ala17]-MCH. As a peptide agonist, its toxicity profile is expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
[Ala17]-MCH is a potent melanin-concentrating hormone (MCH) receptor agonist that is used as a research tool to study the pharmacology of MCH receptors and the physiological roles of the MCH system. It is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C97H155N29O26S4
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|---|---|
| Molecular Weight |
2271.71
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| Exact Mass |
2270.058
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| CAS # |
359784-84-2
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| Related CAS # |
[Ala17]-MCH TFA
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| PubChem CID |
90488845
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.673
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| LogP |
-2.38
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| Hydrogen Bond Donor Count |
32
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| Hydrogen Bond Acceptor Count |
34
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| Rotatable Bond Count |
57
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| Heavy Atom Count |
156
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| Complexity |
4810
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| Defined Atom Stereocenter Count |
18
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| SMILES |
C[C@@H](C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](C(C)C)C(=O)O)NC(=O)[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N2CCC[C@H]2C(=O)N1)CCCNC(=N)N)CC3=CC=C(C=C3)O)C(C)C)CCCNC(=N)N)CC(C)C)CCSC)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CC(=O)O)N
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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, 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: 25 mg/mL (11.00 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (1.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (1.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4402 mL | 2.2010 mL | 4.4020 mL | |
| 5 mM | 0.0880 mL | 0.4402 mL | 0.8804 mL | |
| 10 mM | 0.0440 mL | 0.2201 mL | 0.4402 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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