| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
Neuropathiazol targets pathways involved in neural differentiation, specifically modulating the TGF‑beta/Smad signaling pathway. It indirectly influences the differentiation process by promoting neuronal markers while suppressing glial fate determinants. The compound downregulates the neural progenitor marker Sox2 and upregulates the neuronal marker NeuroD1. It also inhibits astroglial differentiation induced by LIF and BMP2. This modulation of key transcription factors shifts the balance from self‑renewal and glial differentiation toward neuronal commitment in hippocampal progenitor cells.
|
|---|---|
| ln Vitro |
Without causing considerable cytotoxicity, neuropathiazol (5–15 μM; 5-hour exposure) significantly reduces cell growth [1]. Neuropathiazol (10 μM; 1-4 days) increases the marker for neuronal cells, NeuroD1, and downregulates the marker for neural progenitor cells, Sox2 [1]. Additionally, neuropathiazol prevents the differentiation of astrocytes produced by BMP2 and LIF [1]. Multipotent adult hippocampus neural progenitor cells undergo neuronal development when exposed to neuropathiazol [1]. In a dose-dependent manner, neuropathiazol can competitively suppress the synthesis of LIF/BMP2/FBS astrocytes [1].
In HCN neural progenitor cells, Neuropathiazol (5, 10, and 15 μM) significantly slows cell proliferation in a dose‑dependent manner. At 10 μM for 1–4 days, it increases the neuronal marker NeuroD1 and downregulates Sox2. It prevents astrocyte differentiation produced by BMP2 and LIF. The compound competitively suppresses the synthesis of LIF/BMP2/FBS‑induced astrocytes without causing considerable cytotoxicity at 5–15 μM for 5‑hour exposure. It also enhances the maturation of NPC‑derived neurons. |
| ln Vivo |
Neuropathiazol has demonstrated in vivo activity in promoting neuronal differentiation of adult hippocampal neural progenitor cells. It induces neuronal development when multipotent adult hippocampus NPCs are exposed to the compound. The compound is useful for studying stem‑cell fate control processes in vivo. It shows potential for modulating neurogenesis in the adult brain, providing a tool to investigate the mechanisms of neuronal regeneration and differentiation in living organisms.
|
| Enzyme Assay |
In vitro receptor binding assays typically involve incubating purified proteins or membrane preparations with radiolabeled or fluorescently labeled ligands. For Neuropathiazol, competition binding experiments can be performed using hippocampal NPC lysates or recombinant proteins to assess direct interactions. The compound is dissolved in DMSO and diluted in assay buffer (e.g., PBS or Tris‑HCl). Binding affinity (Kd) and IC₅₀ values are determined by nonlinear regression analysis of dose‑response curves. Nonspecific binding is defined using an excess of unlabeled compound. These assays are conducted at room temperature or 4 °C for 1–2 hours, followed by filtration or centrifugation to separate bound from free ligand.
|
| Cell Assay |
Cell proliferation assay[1]
Cell Types: HCN Cell Tested Concentrations: 5 μM, 10 μM, 15 μM Incubation Duration: 5 hrs (hours) Experimental Results: HCN neural progenitor cell proliferation was inhibited. RT-PCR[1] Cell Types: HCN Cell Tested Concentrations: 10 μM Incubation Duration: 1 day, 4 days Experimental Results: Sox2 down-regulated, NeuroD1 up-regulated. HCN hippocampal neural progenitor cells are cultured in standard growth medium (DMEM/F12 with N2 supplement, EGF, and FGF‑2). For proliferation assays, cells are seeded in 96‑well plates and treated with Neuropathiazol at 5, 10, and 15 μM for 5 hours. Cell viability/proliferation is measured using MTT, CCK‑8, or BrdU incorporation assays. For differentiation studies, cells are treated with 10 μM Neuropathiazol for 1–4 days. Gene expression changes are analyzed by RT‑PCR for markers including Sox2 (progenitor) and NeuroD1 (neuronal). Immunocytochemistry with antibodies against βIII‑tubulin (neurons) and GFAP (astrocytes) is used to confirm differentiation. |
| Animal Protocol |
In vivo, Neuropathiazol is typically administered to rodent models via intraperitoneal (IP) or intravenous (IV) injection, or oral gavage. The compound is formulated in a suitable vehicle such as 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline. Dosing regimens may involve daily administration for 1–2 weeks. Endpoints include immunohistochemical analysis of brain tissue for neuronal (NeuN, NeuroD1) and glial (GFAP) markers to assess differentiation. Behavioral tests may be performed to evaluate functional outcomes. Tissue collection and analysis are conducted at specified time points post‑treatment. All procedures follow institutional animal care guidelines.
|
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Neuropathiazol are limited in publicly available sources. Based on its physicochemical properties (LogP 5.74, molecular weight 338.42), the compound is expected to have moderate to high lipophilicity, suggesting good membrane permeability and potential blood‑brain barrier penetration. It shows good solubility in DMSO (50 mg/mL). In vivo, the compound is likely metabolized by hepatic cytochrome P450 enzymes. Further studies are needed to fully characterize its absorption, distribution, metabolism, and excretion (ADME) profile.
|
| Toxicity/Toxicokinetics |
Toxicological data for Neuropathiazol are not extensively reported. In vitro studies indicate that it does not cause considerable cytotoxicity in HCN neural progenitor cells at concentrations up to 15 μM for 5‑hour exposure. Longer‑term exposure effects and in vivo toxicity profiles have not been fully characterized. Standard safety assessments would include acute toxicity studies in rodents, histopathological examination of major organs, and evaluation of hematological and biochemical parameters. The compound is for research use only and not intended for human therapeutic applications.
|
| References |
[1]. Warashina M, et al. A synthetic small molecule that induces neuronal differentiation of adult hippocampal neural progenitor cells. Angew Chem Int Ed Engl. 2006 Jan 16;45(4):591-3.
|
| Additional Infomation |
Neuropathiazol is a research‑grade chemical probe for studying neuronal differentiation mechanisms. Its primary application is in stem cell biology and neurodevelopmental research. The compound is not approved for clinical use and has not entered clinical trials. Its mechanism involves promoting neuronal differentiation while suppressing astrocyte differentiation through modulation of Sox2 and NeuroD1 expression. The compound serves as a tool to investigate the molecular pathways controlling stem‑cell fate. It is available from various chemical suppliers for research purposes only.
|
| Molecular Formula |
C19H18N2O2S
|
|---|---|
| Molecular Weight |
338.42342
|
| Exact Mass |
338.108
|
| CAS # |
880090-88-0
|
| PubChem CID |
11667240
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
517.1±56.0 °C at 760 mmHg
|
| Flash Point |
266.6±31.8 °C
|
| Vapour Pressure |
0.0±1.3 mmHg at 25°C
|
| Index of Refraction |
1.626
|
| LogP |
5.74
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
24
|
| Complexity |
406
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(C1C=CC(N(C)C2=CSC(C3C=CC=CC=3)=N2)=CC=1)OCC
|
| InChi Key |
MGKYEWWFHSESJN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H18N2O2S/c1-3-23-19(22)15-9-11-16(12-10-15)21(2)17-13-24-18(20-17)14-7-5-4-6-8-14/h4-13H,3H2,1-2H3
|
| Chemical Name |
ethyl 4-[methyl-(2-phenyl-1,3-thiazol-4-yl)amino]benzoate
|
| 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 : ~33.33 mg/mL (~98.49 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.39 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 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 (7.39 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 | 2.9549 mL | 14.7745 mL | 29.5491 mL | |
| 5 mM | 0.5910 mL | 2.9549 mL | 5.9098 mL | |
| 10 mM | 0.2955 mL | 1.4775 mL | 2.9549 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
