MIF-1 TFA (Melanostatin) is an endogenous brain peptide and a potent allosteric modulator of dopamine receptors. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation, thereby modulating the analgesic effects of morphine and stress-induced analgesia (SIA). MIF-1 TFA enters the central nervous system/CNS from the blood directly through the BBB (blood-brain barrier).

Physicochemical Properties

Molecular Formula	C15H25F3N4O5
Molecular Weight	398.378014326096
Exact Mass	398.177
CAS #	35240-69-8
Related CAS #	MIF-1;2002-44-0
PubChem CID	137700208
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	5
Hydrogen Bond Acceptor Count	9
Rotatable Bond Count	7
Heavy Atom Count	27
Complexity	454
Defined Atom Stereocenter Count	2
SMILES	CC(C)C[C@@H](C(=O)NCC(=O)N)NC(=O)[C@@H]1CCCN1.C(=O)(C(F)(F)F)O
InChi Key	RNHWSCDHHHUWRY-IYPAPVHQSA-N
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
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
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)

Biological Activity

ln Vitro	MIF-1 TFA (melanostatin, 1 μM) causes spontaneous action potentials to be suppressed and reversibly hyperpolarized[2].
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].
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.
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.

Solubility Data

Solubility (In Vitro)

DMSO: 125 mg/mL (313.77 mM)

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. 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. 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 corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

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.