| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
Glycoprotein 130 (gp130) receptor. UCLA GP130 2 is a potent gp130 receptor agonist and humanin mimetic that binds to the GP130 D4-D5 domain. gp130 is a shared receptor subunit for the interleukin-6 (IL-6) family of cytokines and plays a critical role in neuroprotection, inflammation, and cell survival. Activation of gp130 leads to STAT3 phosphorylation and downstream signaling.
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| ln Vitro |
Within ten minutes of treating SH-SY5Y cells with GP130 receptor agonist-1 (compound 2), there was a two-fold increase in STAT3 phosphorylation at its regulatory Tyr705 site. At all times, pSTAT3 levels in primary hippocampus neuronal cells were lower than the amounts of GP130 receptor agonist-1 that could be detected [1]. In serum-free medium conditions, GP130 receptor agonist-1 treatment of SH-SY5Y cells and primary cortical neurons demonstrated phosphorylation of AKT at its regulatory Thr308 site and ERK1/2 at its Thr202/Tyr204 site. heightened dot phosphorylation [1].
UCLA GP130 2 protects against NMDA-induced toxicity in primary hippocampal neurons in vitro. It increases STAT3 phosphorylation in SH-SY5Y cells. As a humanin mimetic and gp130 receptor agonist, the compound activates gp130-mediated signaling pathways involved in neuroprotection. These effects demonstrate the compound's potential as a neuroprotective agent. The compound's brain-penetrant properties support its use in neurological research. |
| ln Vivo |
Mice were given doses of 10 or 30 mg/kg or 10 mg/kg subcutaneously (SQ) of GP130 receptor agonist-1 (compound 2) at 1, 2, 4, and 6 p.i. and 8 hours after the dose of euthanasia. After two hours of treatment at 10 mg/kg SQ, the brain Cmax was 161 ng/g, and at 30 mg/kg oral dosage, it was 156 ng/g (0.57 μM). For oral dosage of 30 mg/kg and SQ injection of 10 mg/kg, the brain to plasma ratio of 2 is approximately 4:1 and 7.5:1, respectively [1].
UCLA GP130 2 is brain-penetrant and orally active. As a gp130 receptor agonist and humanin mimetic, the compound has potential therapeutic applications in neurodegenerative diseases and conditions involving NMDA-induced excitotoxicity. Its ability to activate gp130/STAT3 signaling suggests neuroprotective effects. Detailed in vivo efficacy data in animal models of neurological disorders are limited in publicly available sources. The compound is primarily used as a research tool for studying gp130 signaling and neuroprotection. |
| Enzyme Assay |
gp130 receptor binding assays are performed using recombinant gp130 receptor protein or using cells expressing gp130. The assay may use radiolabeled or fluorescently labeled ligands to measure binding affinity. Alternatively, functional assays measure gp130-mediated STAT3 phosphorylation in response to agonist stimulation. Test compounds are serially diluted and incubated with gp130 protein or cells for appropriate time periods. Binding affinity (IC50 or Ki) and functional potency (EC50) are determined by non-linear regression. Each concentration is tested in duplicate.
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| Cell Assay |
Cellular gp130 activation is evaluated in SH-SY5Y neuroblastoma cells or primary hippocampal neurons. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with UCLA GP130 2 at various concentrations (0.01-100 μM) for 15-60 minutes. STAT3 phosphorylation (Tyr705) is measured by Western blotting or ELISA. For neuroprotection studies, cells are co-treated with NMDA to induce excitotoxicity, and cell viability is assessed using MTT or LDH assays. Cell death is quantified using propidium iodide staining or calcein-AM staining. Each experiment includes humanin as a positive control and vehicle controls.
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| Animal Protocol |
In vivo efficacy would be evaluated in mouse models of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, stroke) or NMDA-induced excitotoxicity. UCLA GP130 2 is administered orally or intraperitoneally at doses determined by preclinical studies. Behavioral assessments may include tests of motor function, learning and memory, and anxiety-like behavior. Brain tissue is collected for histopathological analysis, STAT3 phosphorylation measurement, and assessment of neuroinflammation and neuronal survival. Sample sizes typically range from 8-12 animals per group. Detailed protocols are not publicly available.
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| ADME/Pharmacokinetics |
UCLA GP130 2 is orally active and brain-penetrant. Molecular weight: 270.32 g/mol. Solubility: DMSO 54 mg/mL (199.76 mM). Purity: ≥98% (HPLC). Storage: +4°C. Bioavailability and half-life data are not publicly available. The compound's brain-penetrant properties suggest good central nervous system exposure following oral administration.
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| Toxicity/Toxicokinetics |
Limited toxicology data are available for UCLA GP130 2. As a gp130 receptor agonist, potential toxicities may include effects on immune function and inflammation. Standard toxicology studies would include acute and subchronic toxicity in rodents, genotoxicity screening, and evaluation of effects on the immune system. No clinical trials have been reported for this compound. The compound is intended for research use only.
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| References | |
| Additional Infomation |
UCLA GP130 2 is also known as GP130 receptor agonist-1 and N-(4-fluorophenyl)-4-phenylthiazol-2-amine. It is a potent, brain-penetrant, and orally active gp130 receptor agonist and humanin mimetic that binds to the GP130 D4-D5 domain and reduces NMDA-induced toxicity. It protects against NMDA-induced toxicity in primary hippocampal neurons and increases STAT3 phosphorylation in SH-SY5Y cells. No clinical trials or regulatory approvals have been reported. The compound is for research use only.
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| Molecular Formula |
C15N2FSH11
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|---|---|
| Molecular Weight |
270.3246
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| Exact Mass |
270.062
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| CAS # |
339303-87-6
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| PubChem CID |
623055
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
424.2±47.0 °C at 760 mmHg
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| Flash Point |
210.3±29.3 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.660
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| LogP |
4.53
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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 |
3
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| Heavy Atom Count |
19
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| Complexity |
275
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)C2=CSC(=N2)NC3=CC=C(C=C3)F
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| InChi Key |
RSKMQDIAPGOWDL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11FN2S/c16-12-6-8-13(9-7-12)17-15-18-14(10-19-15)11-4-2-1-3-5-11/h1-10H,(H,17,18)
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| Chemical Name |
N-(4-fluorophenyl)-4-phenyl-1,3-thiazol-2-amine
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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 (~369.93 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (9.25 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (9.25 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 25.0 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 | 3.6993 mL | 18.4966 mL | 36.9932 mL | |
| 5 mM | 0.7399 mL | 3.6993 mL | 7.3986 mL | |
| 10 mM | 0.3699 mL | 1.8497 mL | 3.6993 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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