[CAS NO. 1229582-33-5] URMC-099
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PRODUCTS SPECIFICATIONS [1229582-33-5]
Store
Catalog
SLK-S7343
Brand
Selleck
CAS
1229582-33-5
DESCRIPTION [1229582-33-5]
Overview
| MDL | MFCD28168077 |
|---|---|
| Molecular Weight | 421.54 |
| Molecular Formula | C27H27N5 |
| SMILES | CN1CCN(CC2=CC=C(C3=CN=C(NC=C4C5=CC6=C(NC=C6)C=C5)C4=C3)C=C2)CC1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3723 mL | 11.8613 mL | 23.7225 mL |
| 5 mM | 0.4745 mL | 2.3723 mL | 4.7445 mL |
| 10 mM | 0.2372 mL | 1.1861 mL | 2.3723 mL |
| 50 mM | 0.0474 mL | 0.2372 mL | 0.4745 mL |
Description
URMC-099 is an orally bioavailable, brain penetrant inhibitor with of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits activity with of 11 nM. URMC-099 also inhibits with IC50 of 6.8 nM. URMC-099 induces .
Targets
In vitro
URMC-099 inhibits LPS-induced TNFα release in microglial cells, and HIV-1 Tat-induced release of cytokines in human monocytes. URMC-099 prevents destruction and phagocytosis of cultured neuronal axons by microglia cells. URMC-099 reduces fMLP-induced chemotaxis of wild-type neutrophil in vitro.
In vivo
In mice, URMC-099 shows excellent pharmacokinetic properties and improved CNS penetration. In vivo, URMC-099 (10 mg/kg i.p.) reduces inflammatory cytokine production, protects neuronal architecture, and alters the morphologic and ultrastructural response of microglia to HIV-1 Tat exposure. URMC099 significantly reduces recruitment of neutrophils into the peritoneum by fMLP in wild-type mice.
References
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