| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| 10mg | ||
| Other Sizes |
| ln Vivo |
Rats' impaired memory brought on by scopolamine was avoided by NNZ 2591 (30 mg/kg; po)[1]. Rats treated with NNZ 2591 (2, 20, 100 ng/rat; icv) exhibit neuroprotection[2]. In rats injured five days later, NNZ 2591 (3 mg/ kg; sc; daily for five days) dramatically lowers the L/R ratio (the amount of time it takes to touch the patch) and fully eliminates brain damage[2].
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|---|---|
| Animal Protocol |
Animal/Disease Models: 4 months, male young adult Wistar rats[1].
Doses: 30 mg/kg Route of Administration: Po; 10 min after the (scopolamine) ip administration. Experimental Results: Dramatically decreased the number of M2AchR positive neurons, Dramatically decreased the density of synaptophysin in the CA3 and CA4 sub-regions , and altered TH terminal staining in the striatum. Animal/Disease Models: 280-310 g adult male Wistar rats[2]. Doses: 2, 20, 100 ng/rat Route of Administration: Icv; 2 h after HI injury Experimental Results: decreased overall tissue damage in the sub-regions of the hippocampus, DG, cerebral cortex and the striatum. Animal/Disease Models: 280-310 g adult male Wistar rats[2]. Doses: 3 mg/kg Route of Administration: Sc; daily for 5 days Experimental Results: Dramatically decreased the median of tissue damage scores in the CA1-2, CA3 and CA4 sub-regions of the hippocampus, the DG. |
| References |
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| Additional Infomation |
NNZ-2591 (cyclic L-glycyl-L-2-allylproline) is an investigational synthetic cyclic glycine-proline (cGP) analogue, a degradation product of human insulin-like growth factor 1 (IGF-1). This analogue has been chemically modified to improve its half-life, stability, and oral bioavailability. Neuren Pharmaceuticals is currently developing this drug for the treatment of symptoms of Angelman syndrome, Phelan-McDermid syndrome, and Pitt Hopkins syndrome. The drug received Orphan Drug Designation from the U.S. Food and Drug Administration (FDA) in October 2019 and a patent from the European Patent Office in December 2019. Clinical trials are expected to begin in 2020.
Mechanism of Action Insulin-like growth factor 1 (IGF-1) is a hormone secreted by glial cells and neurons in the central nervous system (CNS) and plays an important role in normal brain development and pathological responses. In the brain, IGF-1 is broken down into two separate molecules, and synthetic analogs of both are currently under development. Glycine propionate (GPE), composed of the last three peptide segments of IGF-1, acts on glial cells, unlike the parent compound which primarily acts on neurons. A synthetic analog, triphenateline, is currently being developed by Neuren Pharmaceuticals for the treatment of traumatic brain injury, Rett syndrome, and Fragile X syndrome. Glycine propionate is further cleaved into cyclic glycine-proline (cGP), which has multiple functions, including regulating the bioavailability of IGF-1. NNZ-2591 is a synthetic analog of cGP. While the specific mechanism of action of NNZ-2591 may become clearer after clinical trials, IGF-1 and its derivatives are known to regulate responses to disease, stress, and injury through multiple signaling pathways, thereby promoting brain development and normal function. Therefore, any therapeutic effect observed with NNZ-2591 may be the result of multiple different effects rather than the result of action on a specific target. |
| Molecular Formula |
C10H14N2O2
|
|---|---|
| Molecular Weight |
194.23
|
| Exact Mass |
194.105
|
| CAS # |
847952-38-9
|
| PubChem CID |
11735696
|
| Appearance |
White to off-white solid powder
|
| LogP |
0.3
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
14
|
| Complexity |
301
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C([C@@]12CCCN1C(=O)CNC2=O)C=C
|
| InChi Key |
WVKCGUOWPZAROG-JTQLQIEISA-N
|
| InChi Code |
InChI=1S/C10H14N2O2/c1-2-4-10-5-3-6-12(10)8(13)7-11-9(10)14/h2H,1,3-7H2,(H,11,14)/t10-/m0/s1
|
| Chemical Name |
(8aR)-8a-prop-2-enyl-3,6,7,8-tetrahydro-2H-pyrrolo[1,2-a]pyrazine-1,4-dione
|
| 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)
|
| Solubility (In Vitro) |
DMSO: 18.75 mg/mL (96.54 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.5 mg/mL (7.72 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 15.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: 1.5 mg/mL (7.72 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 15.0 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: ≥ 1.5 mg/mL (7.72 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 | 5.1485 mL | 25.7427 mL | 51.4854 mL | |
| 5 mM | 1.0297 mL | 5.1485 mL | 10.2971 mL | |
| 10 mM | 0.5149 mL | 2.5743 mL | 5.1485 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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