| 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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| Other Sizes |
| Targets |
TLXagonist 1 targets the orphan nuclear receptor tailless (TLX, NR2E1). TLX is a transcription factor involved in neural stem cell maintenance, neurogenesis, and brain development. TLXagonist 1 exhibits agonist activity on the human Gal4-fused TLX LBD receptor, resulting in a decrease in reporter activity with an EC₅₀ of 1000 nM. It binds to recombinant TLX protein with a Kd of 650 nM and enhances TLX transcriptional repressive activity.
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|---|---|
| ln Vitro |
In vitro, TLXagonist 1 exhibits agonist activity on the human Gal4-fused TLX LBD receptor, with an EC₅₀ of 1000 nM. It binds to recombinant TLX protein with a Kd of 650 nM. TLXagonist 1 enhances TLX transcriptional repressive activity. The compound is a modulator of the orphan nuclear receptor TLX.
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| ln Vivo |
TLXagonist 1 is not a pharmacologically approved drug. It is a research compound used to study the TLX receptor and its role in neural stem cell maintenance and neurogenesis. The compound has not been evaluated in clinical trials and is not approved for therapeutic use.
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| Enzyme Assay |
In vitro assays for TLXagonist 1 typically involve receptor binding and transcriptional activity studies. A standard protocol for binding studies involves surface plasmon resonance or isothermal titration calorimetry to measure the binding affinity (Kd) of TLXagonist 1 to recombinant TLX protein. For functional assays, cells transfected with a Gal4-fused TLX LBD receptor and a luciferase reporter are treated with varying concentrations of TLXagonist 1 (typically 0.1-100 µM). Luciferase activity is measured after 14 hours. EC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell culture experiments with TLXagonist 1 typically involve neural stem cells or other cells expressing TLX. Cells are cultured in appropriate media and treated with the compound at concentrations ranging from 0.1-100 µM for 24-72 hours. TLX transcriptional activity, gene expression, and cell proliferation are measured.
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| Animal Protocol |
In vivo animal studies with TLXagonist 1 are not well documented, as it is primarily a research compound. If conducted, typical protocols would involve administering the compound to animal models of neurogenesis or brain development. However, such studies are not standard for this compound.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of TLXagonist 1 are not characterized, as it is not a drug substance. Based on its physicochemical properties (molecular weight 374.48, soluble in DMSO at 40 mg/mL), the compound would be expected to have moderate oral bioavailability. However, it is not intended for human exposure.
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| Toxicity/Toxicokinetics |
TLXagonist 1 may cause skin and eye irritation. Standard laboratory safety precautions should be followed when handling this compound, including the use of gloves, safety glasses, and working in a fume hood. The compound should be stored in a cool, dry place away from light and moisture.
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| References | |
| Additional Infomation |
TLXagonist 1 is a modulator of the orphan nuclear receptor tailless (TLX, NR2E1). It exhibits agonist activity with an EC₅₀ of 1000 nM and binds to TLX with a Kd of 650 nM. It has not undergone clinical trials and is not approved as a pharmaceutical.
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| Molecular Formula |
C23H26N4O
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|---|---|
| Molecular Weight |
374.478744983673
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| Exact Mass |
374.21
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| Elemental Analysis |
C, 73.77; H, 7.00; N, 14.96; O, 4.27
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| CAS # |
958323-31-4
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| PubChem CID |
2738508
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| Appearance |
White to off-white solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
489
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=NN1C)C(=O)N2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4
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| InChi Key |
SSGJAUSSGPIZEE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H26N4O/c1-18-17-21(24-25(18)2)23(28)27-15-13-26(14-16-27)22(19-9-5-3-6-10-19)20-11-7-4-8-12-20/h3-12,17,22H,13-16H2,1-2H3
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| Chemical Name |
(4-benzhydrylpiperazin-1-yl)-(1,5-dimethylpyrazol-3-yl)methanone
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| Synonyms |
TLX agonist 1; SUN23314; SUN-23314; SUN 23314; CCRP2; CCRP-2; CCRP 2;
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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: 62.5 mg/mL (166.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.55 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 (5.55 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 (5.55 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 | 2.6704 mL | 13.3518 mL | 26.7037 mL | |
| 5 mM | 0.5341 mL | 2.6704 mL | 5.3407 mL | |
| 10 mM | 0.2670 mL | 1.3352 mL | 2.6704 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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