Pinealon is a 3-amino acid (AA) peptide with neuro-protection properties. Pinealon prevents the accumulation of reactive oxygen species (ROS) and inhibits the activation of ERK 1/2. Pinealon stimulates the functional activity of major cellular components of brain tissue and reduces spontaneous cell death. Pinealon protects rat offspring from prenatal hyperhomocysteinemia.

Physicochemical Properties

Molecular Formula	C15H26N6O8
Molecular Weight	418.40
Exact Mass	418.181
CAS #	175175-23-2
PubChem CID	10273502
Appearance	White to off-white solid powder
LogP	-6.1
Hydrogen Bond Donor Count	8
Hydrogen Bond Acceptor Count	10
Rotatable Bond Count	14
Heavy Atom Count	29
Complexity	649
Defined Atom Stereocenter Count	3
SMILES	C(C[C@@H](C(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)N)CN=C(N)N
InChi Key	QPRZKNOOOBWXSU-CIUDSAMLSA-N
InChi Code	InChI=1S/C15H26N6O8/c16-7(3-4-10(22)23)12(26)21-9(6-11(24)25)13(27)20-8(14(28)29)2-1-5-19-15(17)18/h7-9H,1-6,16H2,(H,20,27)(H,21,26)(H,22,23)(H,24,25)(H,28,29)(H4,17,18,19)/t7-,8-,9-/m0/s1
Chemical Name	(4S)-4-amino-5-[[(2S)-3-carboxy-1-[[(1S)-1-carboxy-4-(diaminomethylideneamino)butyl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic 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
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	In a dose-dependent manner, pinealon (10, 50, and 100 nM; 30 min) inhibits the increase in ROS accumulation in cerebellar granule cells caused by ouabain [1]. Rat cerebellar granule cells exposed to 500 mM homocysteine (HC) are shown to exhibit inhibited ERK 1/2 activation in response to pinealon (10 nM; 0, 2.5, 5, 10, 20, 30 min) [1].
ln Vivo	Pinealon (50, 100, 200 ng/kg; Injection, for 5 days) shows a dose-dependent effect on the maintenance of previously acquired skills in rats[2]. Pinealon (10 µg/kg; daily for 5 days) protects rat offspring from prenatal hyperhomocysteinemia[3].
Animal Protocol	Animal/Disease Models: 200-250 g, white male rats[2] Doses: 50, 100, 200 ng/kg Route of Administration: Injection; for 5 days Experimental Results: demonstrated dose-dependent effects on the maintenance of a previously acquired skill in the Morris maze. Animal/Disease Models: 180-200 g, Female Wistar rats[3] Doses: 10 µg/kg Route of Administration: Ip; daily for 5 days Experimental Results: Protected the rat offspring from prenatal hyperhomocysteinemia.
References	[1]. Pinealon increases cell viability by suppression of free radical levels and activating proliferative processes. Rejuvenation Res. 2011 Oct;14(5):535-41. [2]. Effect of Pinealon on Learning and Expression of NMDA Receptor Subunit Genes in the Hippocampus of Rats with Experimental Diabetes. Neurochemical Journal, 2020, 14, 314-320. [3]. Pinealon protects the rat offspring from prenatal hyperhomocysteinemia. Int J Clin Exp Med. 2012;5(2):179-85.
Additional Infomation	Glu-Asp-Arg is a tripeptide composed of L-glutamic acid, L-aspartic acid, and L-arginine joined in sequence by peptide linkages. It has a role as a neuroprotective agent. It is functionally related to a L-aspartic acid, a L-glutamic acid and a L-arginine.

Solubility Data

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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *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. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.3901 mL	11.9503 mL	23.9006 mL
	5 mM	0.4780 mL	2.3901 mL	4.7801 mL
	10 mM	0.2390 mL	1.1950 mL	2.3901 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.