| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
CCRP2 HCl targets the orphan nuclear receptor tailless (TLX, NR2E1), a key regulator of neural stem cell self-renewal and brain development. It acts as a modulator with an EC50 of 1 μM and a Kd of 650 nM. By enhancing TLX transcriptional repressive activity, it promotes the proliferation and maintenance of neural stem cells.
|
|---|---|
| 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, CCRP2 HCl is characterized as a potent TLX modulator with an EC50 of 1 μM and a Kd of 650 nM. It enhances TLX transcriptional repressive activity. Its activity makes it a valuable tool for studying TLX-mediated signaling pathways in neural stem cells and brain development. |
| ln Vivo |
In vivo, CCRP2 HCl is used as a research tool to study the role of TLX in neural stem cell maintenance and brain development. As a TLX agonist, it can be administered to animal models to study the effects of TLX activation on neurogenesis and brain function. Detailed in vivo pharmacokinetic and efficacy studies are limited.
|
| Enzyme Assay |
In vitro assays for CCRP2 HCl typically involve measuring its binding affinity for TLX and its effects on TLX-mediated transcription. Binding affinity is measured using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Transcriptional activity is assessed using reporter gene assays where cells are transfected with TLX and a reporter plasmid containing TLX response elements.
|
| Cell Assay |
For in vitro cell-based assays, neural stem cells are cultured and treated with CCRP2 HCl at various concentrations. TLX activation is confirmed by measuring the expression of TLX target genes via qRT-PCR. Cell proliferation and self-renewal are assessed by measuring cell number and neurosphere formation. Cell viability is assessed by standard assays.
|
| Animal Protocol |
In vivo animal studies with CCRP2 HCl are conducted in models of neurogenesis and brain development. The compound is administered orally or intraperitoneally. Its effects on neural stem cell proliferation and differentiation are assessed by immunohistochemistry for neural stem cell markers in brain tissues. Behavioral tests can be used to assess cognitive function.
|
| ADME/Pharmacokinetics |
CCRP2 HCl (CAS: 958323-31-4) has a molecular weight of 374.48 g/mol and a molecular formula of C23H26N4O·HCl. Appearance: White to off-white solid powder. Purity: ≥98%. Solubility: DMSO: ~12.5 mg/mL. Storage: Powder -20°C 3 years, 4°C 2 years.
|
| Toxicity/Toxicokinetics |
CCRP2 HCl is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a TLX modulator, it may have effects on neural stem cell proliferation and brain development. Standard laboratory safety precautions should be followed when handling the compound.
|
| References |
|
| Additional Infomation |
CCRP2 HCl (TLX agonist 1, SUN-23314) is a novel and potent modulator of the orphan nuclear receptor tailless (TLX, NR2E1) with an EC50 of 1 μM and a Kd of 650 nM. It enhances TLX transcriptional repressive activity. It has the CAS number 958323-31-4 and a molecular weight of 374.48 g/mol. It is not FDA-approved and is intended for research use only.
|
| Molecular Formula |
C23H26N4O
|
|---|---|
| Molecular Weight |
374.48
|
| CAS # |
958323-31-4
|
| Related CAS # |
958323-31-4;CCRP2 HCl;
|
| PubChem CID |
145925650
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
45
|
| Complexity |
957
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O=C(C1C=C(C)N(C)N=1)N1CCN(C(C2C=CC=CC=2)C2C=CC=CC=2)CC1
|
| InChi Key |
CHQPDKRLUPNGDL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H26N4O.ClH/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,13-16H2,1-2H31H
|
| Chemical Name |
(4-Benzhydrylpiperazin-1-yl)(1,5-dimethyl-1H-pyrazol-3-yl)methanone hydorchloride
|
| Synonyms |
CCRP2 CCRP-2 CCRP 2 CCRP2 HCl CCRP2 hydrochlorideTLX agonist 1
|
| 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
