| Identification | Back Directory | [Name]
UNC3230 | [CAS]
1031602-63-7 | [Synonyms]
UNC3230
2-anilino-5-(cyclohexanecarbonylamino)-1,3-thiazole-4-carboxamide
5-[(Cyclohexylcarbonyl)amino]-2-(phenylamino)-thiazolecarboxamide
4-Thiazolecarboxamide, 5-[(cyclohexylcarbonyl)amino]-2-(phenylamino)- | [Molecular Formula]
C17H20N4O2S | [MDL Number]
MFCD15031190 | [MOL File]
1031602-63-7.mol | [Molecular Weight]
344.43 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
Ethanol:0.2(Max Conc. mg/mL);0.58(Max Conc. mM) | [form ]
A crystalline solid | [color ]
Off-white to light yellow | [InChIKey]
RZCNASHHHSKTGP-UHFFFAOYSA-N | [SMILES]
O=C(N)C1=C(NC(C2CCCCC2)=O)SC(NC3=CC=CC=C3)=N1 |
| Hazard Information | Back Directory | [Description]
Phosphatidylinositol-4-phosphate 5-kinase type-1 γ (PIP5K1C) is a lipid kinase that generates phosphatidylinositol-4,5-bisphosphate (PIP2) in nociceptive dorsal root ganglia (DRG). Pain sensitization is regulated by multiple signaling pathways that are initiated by phospholipase C-mediated hydrolysis of PIP2. UNC3230 is a small molecule inhibitor of PIP5K1C (IC50 = 41 nM, Kd = 51 nM). It does not inhibit any other lipid kinases that regulate phosphoinositide levels, including phosphatidylinositol 3-kinases. At 100 nM, UNC3230 decreases PIP2 membrane levels in cultured DRG neurons by 45% and significantly reduces calcium signaling. At 2 nM, it displays antinociceptive effects in mouse models of chronic pain when administered intrathecally or injected into inflamed hindpaw. | [Uses]
UNC 3230 is a potent inhibitor of PIP5K1C. | [in vivo]
UNC3230 (2 nmol) significantly increases noxious heat-evoked paw withdrawal latency for two hours after intrathecal injection in wild-type mice, indicating an antinociceptive effect[1].
UNC3230 (2 nmol; intrathecal injection) is administered then one hour later co-injected 1 nmol LPA with UNC3230 (2 nmol, intrathecal injection). UNC3230 significantly blunts thermal hyperalgesia and mechanical allodynia compared to vehicle[1].
UNC3230 (2 nmol; intrathecal injection) significantly blunts thermal hyperalgesia and mechanical allodynia in the complete Freund’s adjuvant (CFA)-inflamed hindpaw (relative to vehicle control) but does not affect thermal or mechanical sensitivity in the control (non-inflamed) hindpaw over a multiday time course[1]. | [storage]
Store at +4°C | [References]
[1] BRITTANY D WRIGHT. The lipid kinase PIP5K1C regulates pain signaling and sensitization.[J]. Neuron, 2014: 836-847. DOI: 10.1016/j.neuron.2014.04.006 |
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Lynnchem
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