URMC-099

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 50mg
ArtNr HY-12599-50mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
CAS No.
1229582-33-5
Purity
>98%
MW
4215368
Formula
C27H27N5
Solubility
DMSO: >= 33 mg/mL
Biological Description
URMC-099 is an orally bioavailable, brain penetrant inhibitor of Mixed Lineage Kinase 3(MLK3) with IC50 of 14 nM; inhibits LPS-induced TNFalpha release in microglial cells, HIV-1 Tat-induced release of cytokines in human monocytes, and up-regulation of phospho-JNK in Tat-injected brains of mice.
IC50 value: 14 nM [1]
Target: MLK3 inhibitor
in vitro: URMC-099 shows excellent brain exposure in mouse PK models and minimal interference with key human CYP450 enzymes or hERG channels. inhibits LPS-induced TNFalpha release in microglial cells, HIV-1 Tat-induced release of cytokines in human monocytes and up-regulation of phospho-JNK in Tat-injected brains of mice. URMC-099 likely functions in HAND preclinical models by inhibiting multiple kinase pathways, including MLK3 and LRRK2 (IC50 = 11 nM) [1]. URMC-099 treatment reduced inflammatory cytokine production by HIV-1 Tat-exposed microglia and prevented destruction and phagocytosis of cultured neuronal axons by these cells [2].
in vivo: URMC-099 treatment reduced inflammatory cytokine production, protected neuronal architecture, and altered the morphologic and ultrastructural response of microglia to HIV-1 Tat exposure [2].
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!
Menge: 50mg
Lieferbar: In stock
Listenpreis: 313,57 €
Rabatt: -10,0%
Preis: 282,21 €
Sie sparen: 31,36 €
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