| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
MIF-1 TFA does not target a single receptor but functions as a dopamine receptor allosteric modulator, influencing the response to dopamine. It also inhibits the release of alpha-melanocyte stimulating hormone (alpha-MSH) from the pituitary gland and blocks the effects of opioid receptor activation, modulating analgesic effects.
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| ln Vitro |
MIF-1 TFA (melanostatin, 1 μM) causes spontaneous action potentials to be suppressed and reversibly hyperpolarized[2].
In vitro, MIF-1 TFA has been shown to influence dopamine uptake in crude synaptosomal preparations from rat brain, where it reduces endogenous dopamine content and enhances dopamine uptake kinetics. This supports its role as a modulator of dopaminergic transmission at a presynaptic level. |
| ln Vivo |
MIF-1 TFA (i.p., once, for one hour; male Wistar rats; melanostatin, 1 mg/kg) regulates analgesic effects, including SIA[1]. MIF-1 TFA (melanostatin, 1 mg/kg; intraperitoneal; daily, for 8 weeks; Sprague-Dawley rats) reduces the impairment of striatal dopamine D2 receptor development in rats caused by spiroperidol[3].
In vivo, MIF-1 TFA (20 mg/kg) increases striatal concentrations of dopamine and its metabolites (DOPAC, 3-MT, HVA) in a mouse model. It also antagonizes opioid-induced analgesia and can potentiate the behavioral effects of L-DOPA, enhancing dopamine-mediated behaviors, suggesting it increases nigro-striatal dopaminergic activity. |
| Enzyme Assay |
Non-cellular binding assays for MIF-1 are not standard, as it is an allosteric modulator. Its activity is typically measured in functional assays that assess its ability to alter the binding of orthosteric ligands. For instance, the modulation of [3H]spiperone binding to dopamine D2 receptors in the presence of MIF-1 can be studied, where it allosterically enhances the affinity of the orthosteric antagonist.
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| Cell Assay |
MIF-1 TFA (20 mg/kg) increases the striatal concentration of dopamine and its metabolites in a mouse model of DOPA potentiation. Mice are given MIF-1 followed by L-DOPA, and striatal tissue is analyzed by HPLC-ECD for monoamines. An increase in dopamine levels compared to L-DOPA alone indicates MIF-1‘s dopaminergic effects.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats[1]
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; once, for 1 hour Experimental Results: diminished the analgesic effect. Increased the pain threshold for at least 1 h. Animal/Disease Models: SD (Sprague-Dawley) rats[3] Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; daily, for 8 weeks Experimental Results: Attenuated the ontogenic impairment of striatal D2 receptors that was produced by spiroperidol treatment. An in vivo protocol involves administering MIF-1 (20 mg/kg) to mice, followed by L-DOPA. One hour later, animals are sacrificed, and striatal dopamine, DOPAC, 3-MT, and HVA are measured by HPLC-ECD. A second common protocol uses a tail-flick test for analgesia in rats. MIF-1 is given prior to morphine, and latency to tail flick is measured to assess its ability to block opioid effects. |
| ADME/Pharmacokinetics |
No specific PK data for MIF-1 TFA is provided, but it is known to directly cross the blood-brain barrier (BBB), accessing the central nervous system from the blood. As a peptide, it is generally considered to have a short half-life due to rapid proteolytic degradation unless stabilized, though its BBB permeability is a notable feature.
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| Toxicity/Toxicokinetics |
No detailed toxicological data is provided. MIF-1 TFA has been investigated in clinical studies for Parkinson's disease, tardive dyskinesia, and depression, and is generally reported to be well-tolerated with a good safety profile. Potential adverse effects are mild and may be related to its dopaminergic or hormonal modulatory effects.
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| References |
[1]. Bocheva A, et, al. Antiopioid properties of the TYR-MIF-1 family. Methods Find Exp Clin Pharmacol. 2004 Nov;26(9):673-7.
[2]. Valentijn JA, et, al. Melanostatin (NPY) inhibited electrical activity in frog melanotrophs through modulation of K+, Na+ and Ca2+ currents. J Physiol. 1994 Mar 1;475(2):185-95. [3]. Saleh MI, et, al. MIF-1 attenuates spiroperidol alteration of striatal dopamine D2 receptor ontogeny. Peptides. 1989 Jan-Feb;10(1):35-9. |
| Additional Infomation |
MIF-1 TFA is one of the few endogenous peptides that has been extensively studied for its clinical potential. It has been evaluated for Parkinson‘s disease, treatment-resistant depression, and to attenuate levodopa-related dyskinesias. Its ability to cross the BBB and modulate central dopaminergic tone without directly binding to receptor orthosteric sites makes it a unique therapeutic concept.
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| Molecular Formula |
C15H25F3N4O5
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|---|---|
| Molecular Weight |
398.378014326096
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| Exact Mass |
398.177
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| CAS # |
35240-69-8
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| Related CAS # |
MIF-1;2002-44-0
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| PubChem CID |
137700208
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
454
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)C[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1.C(=O)(C(F)(F)F)O
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| InChi Key |
RNHWSCDHHHUWRY-IYPAPVHQSA-N
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| InChi Code |
InChI=1S/C13H24N4O3.C2HF3O2/c1-8(2)6-10(12(19)16-7-11(14)18)17-13(20)9-4-3-5-15-9;3-2(4,5)1(6)7/h8-10,15H,3-7H2,1-2H3,(H2,14,18)(H,16,19)(H,17,20);(H,6,7)/t9-,10-;/m0./s1
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| Chemical Name |
(2S)-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide;2,2,2-trifluoroacetic acid
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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) |
DMSO: 125 mg/mL (313.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.22 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 20.8 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: ≥ 2.08 mg/mL (5.22 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 20.8 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: ≥ 2.08 mg/mL (5.22 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 | 2.5102 mL | 12.5508 mL | 25.1017 mL | |
| 5 mM | 0.5020 mL | 2.5102 mL | 5.0203 mL | |
| 10 mM | 0.2510 mL | 1.2551 mL | 2.5102 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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