GENZ-882706 (RA03546849) (Synonyms: RA03546849) |
| رقم الكتالوجGC31842 |
GENZ-882706 (RA03546849) هو مثبط قوي لمستقبل العامل -1 (CSF-1R) المستخرج من براءة الاختراع WO 2017015267A1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2070864-35-4
Sample solution is provided at 25 µL, 10mM.
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GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1.
Genz-882706 induces an increased level of proliferative activity on unstimulated cells 48 hours post treatment and the reason for this effect is unclear[1].
Daily treatment with Genz-882706 significantly reduces experimental autoimmune encephalomyelitis. Treatment with Genz-882706 in experimental autoimmune encephalomyelitis (EAE) mice results in significant decreases in MCP-1, IL-6, IL-Ιβ and IP-10 levels in spinal cord homogenates when compared to Vehicle treated animals. Treatment with Genz-882706 shows a significant increase in TNF-a levels in the spinal cord when compared to the vehicle treated group. Genz-882706 at both the 30 mg/kg and the 100 mg/kg dose significantly reduces the number of microglia and monocytes/macrophages in the brain and spinal cord compared to the vehicle and LPS controls. Treatment with Genz-882706 modestly reduces CD80 expression on monocytes/macrophages in the brain[1].
[1]. Kane, et al. Colony Stimulating Factor-1 Receptor (CSF-1R) Inhibitors. WO 2017015267A1
Cell experiment: | To determine the effect of GENZ-882706 on the proliferation of primary murine microglial cells following LPS or CSF-1 stimulation, GENZ-882706 (500 nM) is added to appropriate assay wells. 25 μL medium are also added to all cells only wells at this time. 25 μL of LPS at 10 ng/mL or 100 ng/mL or CSF-1 at 100 ng/mL are then added to appropriate wells. 25 μL of medium are added to wells not receiving LPS or CSF-1 to bring the final volume of all assay wells to 150uL[1]. |
Animal experiment: | Mice[1]Mycobacterium tuberculosis is induced in a secondary progressive experimental autoimmune encephalomyelitis (EAE) model in NOD mice with an emulsion of MOG 35-55 and CFA. Therapeutic treatment with Genz-882706 (25mg/kg/day) or vehicle control is started on Day 27 post-disease induction when mice began to enter the progressive stage of disease. Inflammatory/neurotoxic mediators in the CNS are measured through protein analysis in homogenate and gene expression[1]. |
References: [1]. Kane, et al. Colony Stimulating Factor-1 Receptor (CSF-1R) Inhibitors. WO 2017015267A1 | |
| Cas No. | 2070864-35-4 | SDF | |
| المرادفات | RA03546849 | ||
| Canonical SMILES | COC1=CC=C([C@@H]2OC(C=CC(CN3C4=NC=C(C#CC(N)(C)C)C=C4N=C3)=C5)=C5OC2)C=N1 | ||
| Formula | C26H25N5O3 | M.Wt | 455.51 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1953 mL | 10.9767 mL | 21.9534 mL |
| 5 mM | 0.4391 mL | 2.1953 mL | 4.3907 mL |
| 10 mM | 0.2195 mL | 1.0977 mL | 2.1953 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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