| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
GPI-1485 targets immunophilins, specifically FKBP52 (FK506-binding protein 52), a peptidyl-prolyl cis-trans isomerase. Unlike FK506, which has immunosuppressive effects through FKBP12 and calcineurin inhibition, GPI-1485 selectively binds to FKBP52 and retains neuroprotective activity without immunosuppressive side effects. The compound promotes neurofunctional improvement and neural regeneration through neurotrophic factor-like activity. The molecular targets and pathways involved include the peptidyl-prolyl cis-trans isomerase FKBP1A, which plays a role in neuroprotection.
|
|---|---|
| ln Vitro |
Normal human dermal fibroblasts (NHDF) undergo cellular reprogramming and neural activation upon exposure to GPI-1485 (GM1485; 100 μM) [1].
In vitro studies show that GPI-1485 (100 μM) induces cell reprogramming and neural cell induction in normal human dermal fibroblasts (NHDF). The compound promotes neurofunctional improvement and neural regeneration through neurotrophic activity. As a non-immunosuppressive immunophilin ligand, GPI-1485 retains neuroprotective activity without immunosuppressive effects. The compound's neurotrophic activity leads to the repair and regeneration of damaged nerves. In cellular assays, GPI-1485 promotes neuronal survival and neurite outgrowth. |
| ln Vivo |
In intraperitoneal injection given daily for six weeks, GPI-1485 (GM1485; 5 mg/kg) enhances rats' long-term neurological recovery [1].
In vivo studies demonstrate that GPI-1485 promotes neurofunctional improvement and neural regeneration following stroke. GPI-1485 (5 mg/kg; intraperitoneal injection; once daily for 6 weeks) significantly promoted long-term neural recovery in rats. The compound has been investigated for use in Parkinson's disease and erectile dysfunction. GPI-1485 is commonly used in research on neurofunctional impairment and regeneration in neurodegenerative diseases. The compound's ability to promote neural regeneration without immunosuppression makes it attractive for neurological research. |
| Enzyme Assay |
The in vitro receptor binding assay for GPI-1485 involves measuring FKBP52 binding affinity. Recombinant FKBP52 is incubated with varying concentrations of GPI-1485 (1 nM-100 μM) and a fixed concentration of radiolabeled FK506 or other FKBP ligand. Non-specific binding is determined using excess unlabeled FK506. IC50 values are calculated from competition binding curves. Peptidyl-prolyl cis-trans isomerase activity of FKBP52 is measured using a chymotrypsin-coupled protease assay with a peptide substrate. The compound's effect on isomerase activity is assessed. Selectivity for FKBP52 over FKBP12 is confirmed by comparing binding affinities.
|
| 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. In vitro cellular assays for GPI-1485 typically use neuronal cell lines (e.g., SH-SY5Y, PC12) or primary neurons. Cells are cultured in appropriate media and treated with the compound at concentrations of 1-100 μM for 24-72 hours. Neurite outgrowth is assessed by microscopy. Neuronal survival is evaluated using MTT or LDH release assays. For fibroblast reprogramming studies, normal human dermal fibroblasts (NHDF) are treated with the compound at 100 μM. Neural marker expression (Nestin, MAP2, etc.) is analyzed by immunofluorescence or Western blot. Neurotrophic factor production is measured by ELISA. |
| 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. In vivo animal studies for GPI-1485 involve rat models of stroke or neurodegenerative disease. Rats are treated with the compound via intraperitoneal injection at 5 mg/kg, once daily for up to 6 weeks. Neurological function is assessed using behavioral tests (e.g., modified neurological severity scores, rotarod test). Lesion volume is measured by histology or MRI. Neural regeneration is assessed by immunohistochemistry for neural markers (NeuN, GFAP). For Parkinson's disease models, MPTP-treated mice are used. Behavioral tests and dopaminergic neuron survival are assessed. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of GPI-1485 indicate the compound is suitable for systemic administration. The compound has a molecular weight of 269.34 and molecular formula of C12H19NO5?. It is soluble in DMSO and other organic solvents. The compound should be stored at -20°C for long-term preservation. After intraperitoneal or oral administration, the compound reaches systemic circulation and distributes to tissues including the brain. The duration of neuroprotective activity is consistent with the compound's half-life. Further studies on plasma half-life, clearance, and protein binding are needed.
|
| Toxicity/Toxicokinetics |
Toxicological data for GPI-1485 indicates a favorable safety profile compared to immunosuppressive immunophilins. The compound retains neuroprotective activity without immunosuppressive side effects, suggesting reduced toxicity. The compound is for research use only and not for human therapeutic applications. Standard safety precautions should be followed when handling. For detailed toxicity information, specialized toxicological studies would need to be performed.
|
| References | |
| Additional Infomation |
GPI 1485 is a candidate product belonging to a class of small molecule compounds called neuroimmunavidin ligands. Preclinical studies have shown that neuroimmunavidin ligands can repair and regenerate damaged nerves without affecting normal healthy nerves. GPI 1485 is currently in a Phase II clinical trial for the treatment of Parkinson's disease and erectile dysfunction after prostatectomy, and is also undergoing preclinical development for HIV-related dementia and neuropathy.
Drug Indications It is being investigated for the treatment of erectile dysfunction and Parkinson's disease. Mechanism of Action GPI 1485 belongs to a class of small molecule compounds called neuroimmunavidin ligands, which are highly conserved binding proteins that mediate the effects of immunosuppressants. The FK-506-binding protein (FKBP) subclass of immunoavidins can bind to FK-506 and rapamycin and has attracted attention due to its potent neurotrophic activity. GPI-1485 (GM1485) is a research-grade compound with CAS number 186268-78-0. It is a non-immunosuppressive neuroimmunophilin ligand derived from FK506. The compound selectively binds to FKBP52 and retains neuroprotective activity. It promotes neurofunctional improvement and neural regeneration following stroke. The compound has been investigated for Parkinson's disease and erectile dysfunction. Its mechanism involves neurotrophic factor-like activity and neural regeneration. It has not been FDA-approved and is strictly for research purposes only. |
| Molecular Formula |
C12H19NO4
|
|---|---|
| Molecular Weight |
241.287
|
| Exact Mass |
241.131
|
| CAS # |
186268-78-0
|
| PubChem CID |
9837656
|
| Appearance |
White to light yellow solid powder
|
| Density |
1.189 g/cm3
|
| Boiling Point |
386.198ºC at 760 mmHg
|
| Flash Point |
187.366ºC
|
| LogP |
1.005
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
17
|
| Complexity |
348
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CCC(C)(C)C(=O)C(=O)N1CCC[C@H]1C(=O)O
|
| InChi Key |
FOPALECPEUVCTL-QMMMGPOBSA-N
|
| 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
|
| Synonyms |
GPI1485; GPI 1485; GPI-1485
|
| 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 : ~100 mg/mL (~414.46 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
