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AB287145

PLX5622 (free base)

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MW 395.4 Da, Purity >98%. Inhibitor of colony-stimulating factor 1 receptor (CSF1R) tyrosine kinase with a Ki of 5.9 nM. It causes sustained and specific elimination of microglia. As a result of microglial depletion, plaques fail to form in the parenchymal space in the 5xFAD mouse model of Alzheimer's disease (AD). Inhibition of the CSF1R at lower doses in 3xTg-AD mice prevents microglial association with plaques and improves cognition.

View Alternative Names

(R)-limonene 6-monooxygenase, (S)-limonene 6-monooxygenase, (S)-limonene 7-monooxygenase, 1,8-cineole 2-exo-monooxygenase, Albendazole monooxygenase, Albendazole sulfoxidase, C-FMS, CD 115, CD115 antigen, CP2C9_HUMAN, CP33, CP34, CP3A4_HUMAN, CPC9, CSF-1 receptor, CSF1R_HUMAN, CSFR, CYP2C, CYP2C10, CYP2C19, CYP3, CYP3A, CYP3A3, CYP3A4, CYPIIC17, CYPIIC19, CYPIIC9, CYPIIIA3, CYPIIIA4, Colony stimulating factor 1 receptor, Colony stimulating factor I receptor, Cytochrome P-450MP, Cytochrome P450 2C19, Cytochrome P450 2C9, Cytochrome P450 3A3, Cytochrome P450 3A4, Cytochrome P450 HLp, Cytochrome P450 MP-4, Cytochrome P450 MP-8, Cytochrome P450 NF-25, Cytochrome P450 PB-1, Cytochrome P450 family 3 subfamily A polypeptide 4, Cytochrome P450 subfamily IIIA polypeptide 4, Cytochrome P450, family 2, subfamily C, polypeptide 9, Cytochrome P450-11A, Cytochrome P450-254C, Cytochrome P450-PCN1, EC 2.7.10.1, FIM 2, FMS, FMS proto oncogene, Glucocorticoid inducible P450, HDLS, HLP, M-CSF Receptor, M-CSF-R, MGC126680, MGC149605, MGC88320, Macrophage colony stimulating factor I receptor, Macrophage colony-stimulating factor 1 receptor, McDonough feline sarcoma viral (v fms) oncogene homolog, Mephenytoin 4-hydroxylase, Microsomal monooxygenase, NF 25, Nifedipine oxidase, OTTHUMP00000020135, Oncogen FMS, P450 III steroid inducible, P450 MP, P450 PB 1, P450 PCN1, P450, family III, P450C3, P450IIC9, Proto-oncogene c-Fms, Quinine 3-monooxygenase, S-mephenytoin 4-hydroxylase, Taurochenodeoxycholate 6-alpha-hydroxylase, V-FMS McDonough feline sarcoma viral oncogen homolog, formerly, Xenobiotic monooxygenase, cytochrome P-450 S-mephenytoin 4-hydroxylase, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, flavoprotein-linked monooxygenase

Key facts

CAS number

1303420-67-8

Purity

>98%

Form

Solid

form

Molecular weight

395.4 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>1</sub><sub>9</sub>F<sub>2</sub>N<sub>5</sub>O

PubChem

52936034

Nature

Synthetic

Solubility

Soluble in DMSO

Biochemical name

6-Fluoro-N-((5-fluoro-2-methoxypyridin-3-yl)methyl)-5-((5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2-amine

Biological description

Inhibitor of colony-stimulating factor 1 receptor (CSF1R) tyrosine kinase with a Ki of 5.9 nM. It causes sustained and specific elimination of microglia. As a result of microglial depletion, plaques fail to form in the parenchymal space in the 5xFAD mouse model of Alzheimer's disease (AD). Inhibition of the CSF1R at lower doses in 3xTg-AD mice prevents microglial association with plaques and improves cognition.

Canonical smiles

CC1=CC2=C(NC=C2CC3=C(N=C(C=C3)NCC4=C(N=CC(=C4)F)OC)F)N=C1

InChi

InChI=1S/C21H19F2N5O/c1-12-5-17-14(9-26-20(17)25-8-12)6-13-3-4-18(28-19(13)23)24-10-15-7-16(22)11-27-21(15)29-2/h3-5,7-9,11H,6,10H2,1-2H3,(H,24,28)(H,25,26)

InChiKey

NSMOZFXKTHCPTQ-UHFFFAOYSA-N

IUPAC Name

6-fluoro-N-[(5-fluoro-2-methoxypyridin-3-yl)methyl]-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-amine

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Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2965 PLX5622 (free base). B2965-5 is the same size as the 5 mg size of ab287145.
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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Cytochrome P450 3A4 commonly known as CYP3A4 is an important enzyme in the cytochrome P450 family. It possesses a molecular mass of approximately 57 kDa. This enzyme mainly expresses in the liver and the small intestine. CYP3A4 belongs to the class of proteins responsible for oxidizing small organic molecules which is essential for the metabolism of a range of xenobiotics and endogenous compounds. Various substrates including medications toxins and metabolic products undergo modification by CYP3A4 impacting their activity and clearance from the body.
Biological function summary

Cytochrome P450 3A4 performs a significant role in the body's xenobiotic metabolism process. It is a component of a larger protein complex that includes NADPH-P450 reductase. This enzyme is involved in the oxidation of organic substances including steroids and fatty acids. Its activity affects drug metabolism influencing the pharmacokinetics and pharmacodynamics of many therapeutic drugs. CYP3A4's modulation can have far-reaching implications on bioavailability and toxicity levels in diverse cellular environments.

Pathways

CYP3A4 is intricately involved in the metabolism of both endogenous and exogenous compounds within the cytochrome P450 pathway. This pathway includes processes such as drug detoxification and hormone synthesis. In these processes CYP3A4 interacts with several other cytochrome P450 enzymes such as CYP2C9 and CYP2C19 to metabolize various substrates. The enzyme also plays a role in the mevalonate pathway which is important for cholesterol biosynthesis therefore connecting it to broader biological processes.

CYP3A4's activity influences several conditions including liver disease and drug-induced toxicity. Its expression level changes can affect drug efficacy and potential adverse reactions. A decreased activity of CYP3A4 can lead to accumulation of drugs and increased risk of side effects while increased activity might reduce drug effectiveness. CYP3A4 closely interacts with the colony-stimulating factor 1 receptor (CSF-1-R) in these contexts linking it to processes of inflammation and cellular proliferation which are vital in cancer and liver fibrosis.
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Product protocols

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