| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Normal human dermal fibroblasts (NHDF) undergo cellular reprogramming and neural activation upon exposure to GPI-1485 (GM1485; 100 μM) [1].
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|---|---|
| ln Vivo |
In intraperitoneal injection given daily for six weeks, GPI-1485 (GM1485; 5 mg/kg) enhances rats' long-term neurological recovery [1].
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| Cell Assay |
Cell viability assay[1]
Cell Types: Normal human dermal fibroblasts (NHDF)[1] Tested Concentrations: 100 μM Incubation Duration: Experimental Results: Induced cell reprogramming and neural cell induction. |
| Animal Protocol |
Animal/Disease Models: Adult male Wistar rats, body weight 250-300 g[1]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; 42 days in total Experimental Results: Administration improved neurological function, compared with rats after stroke Consistent upregulation of endogenous neurogenesis. |
| References | |
| Additional Infomation |
GPI 1485 is a product candidate that belongs to a class of small molecule compounds called neuroimmunophilin ligands. In preclinical experiments, neuroimmunophilin ligands have been shown to repair and regenerate damaged nerves without affecting normal, healthy nerves. GPI 1485 is being studied in phase 2 clinical trials for the treatment of Parkinson's disease and post-prostatectomy erectile dysfunction and in pre-clinical development for HIV related dementia and neuropathy.
Drug Indication Investigated for use/treatment in erectile dysfunction and parkinson's disease. Mechanism of Action GPI 1485 belongs to a class of small molecule compounds called neuroimmunophilin ligands which are a family of binding proteins that are highly conserved in nature and mediate the actions of immunosuppressant drugs. The FK-506-binding protein (FKBP) subclass of immunophilin bind FK-506 and rapamycin and are of particular interest due to their potent neurotrophic activity. |
| Molecular Formula |
C12H19NO4
|
|---|---|
| Molecular Weight |
241.287
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| Exact Mass |
241.131
|
| CAS # |
186268-78-0
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| PubChem CID |
9837656
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| Appearance |
White to light yellow solid powder
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| Density |
1.189 g/cm3
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| Boiling Point |
386.198ºC at 760 mmHg
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| Flash Point |
187.366ºC
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| LogP |
1.005
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
348
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| Defined Atom Stereocenter Count |
1
|
| SMILES |
CCC(C)(C)C(=O)C(=O)N1CCC[C@H]1C(=O)O
|
| InChi Key |
FOPALECPEUVCTL-QMMMGPOBSA-N
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| InChi Code |
InChI=1S/C12H19NO4/c1-4-12(2,3)9(14)10(15)13-7-5-6-8(13)11(16)17/h8H,4-7H2,1-3H3,(H,16,17)/t8-/m0/s1
|
| Chemical Name |
(2S)-1-(3,3-dimethyl-2-oxopentanoyl)pyrrolidine-2-carboxylic acid
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| Synonyms |
GPI1485; GPI 1485; GPI-1485
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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 |
| 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 : ~100 mg/mL (~414.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.62 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 (8.62 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 (8.62 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 | 4.1444 mL | 20.7220 mL | 41.4439 mL | |
| 5 mM | 0.8289 mL | 4.1444 mL | 8.2888 mL | |
| 10 mM | 0.4144 mL | 2.0722 mL | 4.1444 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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