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  3. GENZ-882706

GENZ-882706 (Synonyms: RA03546849)

Cat. No.: HY-101526
Handling Instructions

GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1.

For research use only. We do not sell to patients.

GENZ-882706 Chemical Structure

GENZ-882706 Chemical Structure

CAS No. : 2070864-35-4

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Description

GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1.

IC50 & Target

Target: CSF-1R[1]

In Vitro

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].

In Vivo

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].

Molecular Weight

455.51

Formula

C₂₆H₂₅N₅O₃

CAS No.

2070864-35-4

SMILES

COC1=CC=C([[email protected]@H]2OC(C=CC(CN3C4=NC=C(C#CC(N)(C)C)C=C4N=C3)=C5)=C5OC2)C=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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KeyWords:

GENZ-882706 | RA03546849 | GENZ882706 | GENZ 882706 | RA 03546849 | RA-03546849 | c-Fms | CSF-1 receptor | colony stimulating factor 1 receptor | CSF-1R | CSF1R | Inhibitor | inhibitor | inhibit

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GENZ-882706
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