| Identification | Back Directory | [Name]
(S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one | [CAS]
2049868-46-2 | [Synonyms]
GSK'963
GSK-963;GSK 963;GSK'963
(S)-2,2-dimethyl-1-(5-phenyl-4,5-dihydro-1H-pyrazol-1-yl)propan-1-one
1-Propanone, 1-[(5S)-4,5-dihydro-5-phenyl-1H-pyrazol-1-yl]-2,2-dimethyl- | [Molecular Formula]
C14H18N2O | [MDL Number]
MFCD31813620 | [MOL File]
2049868-46-2.mol | [Molecular Weight]
230.31 |
| Chemical Properties | Back Directory | [Boiling point ]
342.8±45.0 °C(Predicted) | [density ]
1.06±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 25 mg/mL (108.55 mM; Need ultrasonic) | [form ]
Solid | [pka]
0.98±0.40(Predicted) | [color ]
Light yellow to yellow | [SMILES]
O=C(C(C)(C)C)N1[C@H](C2=CC=CC=C2)CC=N1 |
| Hazard Information | Back Directory | [Uses]
GSK''963 is a novel highly potent and selective RIP1 inhibitor. | [Biological Activity]
GSKμ963 (GSKμ963A) is a brain-penetranthighly potent and selective ATP site-targeting receptor-interacting protein 1 kinase (RIP1; RIPK1) inhibitor (IC50 = 0.8-8 nM with 50 μM ATP; IC50 >10 μM against RIPK2/3/5 and 335 other kinases) th at protects against TNFα/zVAD-induced necroptosis (EC50 = 1/4 nM in mouse L929/human U937 cultures) and blocks Y. pestis-induced death of murine fetal liver macrophages (1 μM). GSKμ963 prevents lethal hypothermia by acute sterile shock (2 mg/kg i.p. 15 min prior to TNFα/zVAD i.v.) and protects against acute neuronal death upon autologous blood intracerebral hemorrhage induction in mice in vivo (25 mg/kg/3 hr i.p.). | [in vivo]
GSK963 (2 mg/kg) results in a complete protection from TNF+zVAD-induced temperature loss. GSK963 (0.2 mg/kg) also shows a significant response[1]. | Animal Model: | C57BL/6 mice[1]. | | Dosage: | 0.2 mg/kg, 2 mg/kg, 10?mg/kg. | | Administration: | IP once. | | Result: | Protected mice from TNF+zVAD-induced hypothermia. |
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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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