| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
CCRP2 targets the orphan nuclear receptor tailless (TLX, NR2E1), a transcription factor that plays a critical role in neural stem cell self-renewal, neurogenesis, and brain development. CCRP2 binds to recombinant TLX protein with a Kd of 650 nM and has an EC50 of 1.0 µM for modulating TLX activity. It enhances TLX transcriptional repression activity. By modulating TLX activity, CCRP2 can influence the proliferation, differentiation, and maintenance of neural stem cells. The compound is a valuable tool for studying the role of TLX in neural development and for exploring the therapeutic potential of targeting TLX in neurological disorders.
|
|---|---|
| ln Vitro |
BMS-1001 attaches itself to human PD-L1 and prevents it from interacting with PD-1. BMS-1001 exhibits minimal toxicity towards the cell lines examined and inhibits the communication between soluble PD-L1 and cell surface-expressed PD-1. The inhibitory effect of soluble PD-L1 on T cell receptor-mediated T lymphocyte activation is lessened by BMS-1001 [1].
In vitro studies have demonstrated that CCRP2 binds to recombinant TLX protein with a Kd of 650 nM and enhances TLX transcriptional repression activity. It has an EC50 of 1.0 µM for modulating TLX activity. These in vitro findings confirm the compound's activity as a TLX modulator. CCRP2 is used in cell-based assays to study the effects of TLX modulation on neural stem cell proliferation, differentiation, and gene expression. The compound is a valuable tool for studying the role of TLX in neural stem cell biology, neurogenesis, and brain development. However, specific detailed in vitro data beyond its binding and activity are not extensively documented. |
| ln Vivo |
In vivo studies on CCRP2 are limited, as the compound is primarily used as a research tool for studying TLX biology. As a TLX modulator, CCRP2 has the potential to influence neural stem cell function and neurogenesis in vivo. However, specific in vivo data for CCRP2, including efficacy in animal models and pharmacokinetic parameters, are not extensively documented in publicly available sources. The compound is primarily used in research to study the role of TLX in neural development and to explore the therapeutic potential of targeting TLX in neurological disorders. Research-grade CCRP2 is intended for laboratory use only.
|
| Enzyme Assay |
Non-cellular binding assays for CCRP2 typically involve measuring its affinity for the orphan nuclear receptor TLX (NR2E1) using radioligand binding or fluorescence polarization techniques. The compound is tested at various concentrations in the presence of a labeled reference ligand to determine its Kd for TLX binding. Assays are performed in buffer systems at physiological pH and temperature, with incubation times optimized for equilibrium binding. Non-specific binding is determined in the presence of excess unlabeled ligand. Kd values are calculated using binding curves and non-linear regression analysis. These assays are essential for characterizing the binding affinity and potency of CCRP2 for TLX.
|
| Cell Assay |
In vitro cell-based assays for CCRP2 typically use cell lines expressing TLX, such as neural stem cells or cell lines transfected with TLX, to assess the compound's effects on TLX activity and gene expression. Cells are cultured in appropriate media and treated with CCRP2 at various concentrations. TLX activity is assessed by measuring the expression of reporter genes under the control of TLX response elements or by measuring the expression of TLX target genes by qRT-PCR. Cell proliferation and differentiation are assessed using standard assays. Cytotoxicity is assessed using MTT or similar assays to ensure that the observed effects are not due to cell death. CCRP2 is typically dissolved in DMSO and diluted in culture medium, with DMSO controls included to account for solvent effects.
|
| Animal Protocol |
In vivo animal studies for CCRP2 would typically involve mouse models of neurological disorders or models for studying neural stem cell biology. Animals would be treated with CCRP2 at various doses, typically administered orally or intraperitoneally. Neurogenesis, brain development, and behavior would be assessed. However, specific published in vivo data for CCRP2 are not extensively documented. The compound is primarily used as a research tool for studying TLX biology and as a lead compound for the development of TLX-targeted therapies. Further studies are needed to validate its in vivo efficacy.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for CCRP2 are limited in publicly available sources. The compound has a molecular weight of 374.48 g/mol and a molecular formula of C23H26N4O. As a small molecule, CCRP2 is expected to be absorbed and distributed to tissues. However, detailed PK parameters such as half-life, Cmax, AUC, and bioavailability have not been extensively reported. The compound's solubility and stability are important factors for its use in in vitro and in vivo studies. Research-grade CCRP2 is intended for laboratory use only. Further pharmacokinetic studies are needed to fully characterize the compound's absorption, distribution, metabolism, and excretion.
|
| Toxicity/Toxicokinetics |
Toxicological data for CCRP2 are limited. As a research compound, CCRP2 is intended for laboratory use only and is not for human consumption. Standard toxicological assessments, including acute and chronic toxicity studies, would be required for clinical development. However, these data are not publicly available. In vitro studies suggest that CCRP2 can be used at concentrations that effectively modulate TLX activity without causing significant cytotoxicity. The compound's safety profile in vivo has not been extensively characterized. As with all research chemicals, appropriate safety precautions should be taken when handling CCRP2.
|
| References |
|
| Additional Infomation |
CCRP2 (TLX agonist 1; SUN23314) is a modulator of the orphan nuclear receptor tailless (TLX, NR2E1). It has the CAS number 958323-31-4. CCRP2 has an EC50 of 1.0 µM and a Kd of 650 nM for TLX and enhances TLX transcriptional repression activity. CCRP2 is not approved for clinical use and is strictly a research compound for studying TLX biology in neural stem cell and neurogenesis research.
|
| Molecular Formula |
C23H26N4O
|
|---|---|
| Molecular Weight |
374.48
|
| Exact Mass |
374.21
|
| Elemental Analysis |
C, 73.77; H, 7.00; N, 14.96; O, 4.27
|
| CAS # |
958323-31-4
|
| Related CAS # |
958323-31-4;CCRP2 HCl;
|
| Appearance |
White to off-white solid powder
|
| LogP |
0
|
| SMILES |
O=C(C1C=C(C)N(C)N=1)N1CCN(C(C2C=CC=CC=2)C2C=CC=CC=2)CC1
|
| InChi Key |
SSGJAUSSGPIZEE-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
(4-benzhydrylpiperazin-1-yl)(1,5-dimethyl-1H-pyrazol-3-yl)methanone
|
| Synonyms |
TLX agonist 1 CCRP2 CCRP-2 CCRP 2
|
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~12.5 mg/mL (~19.81 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.98 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 12.5 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: ≥ 1.25 mg/mL (1.98 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 12.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA