| Identification | Back Directory | [Name]
CAY10618 | [CAS]
1202580-59-3 | [Synonyms]
GPP 78
CAY10618
CAY10618 Exclusive
N-(2-phenylphenyl)-8-(4-pyridin-3-yltriazol-1-yl)octanamide
1H-1,2,3-Triazole-1-octanaMide, N-[1,1'-biphenyl]-2-yl-4-(3-pyridinyl)- | [Molecular Formula]
C27H29N5O | [MOL File]
1202580-59-3.mol | [Molecular Weight]
439.55 |
| Chemical Properties | Back Directory | [density ]
1.15±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml; Ethanol: 10 mg/ml | [form ]
Liquid | [pka]
14.80±0.70(Predicted) | [color ]
Colorless to light yellow |
| Hazard Information | Back Directory | [Description]
Nicotinamide phosphoribosyltransferase (Nampt) converts nicotinamide into nicotinamide mononucleotide (NMN), which is subsequently converted to NAD+ by NMN adenyltransferase. Cancer cells commonly have an unusually high rate of NAD+ turnover, suggesting that inhibition of Nampt might selectively target cancer cells. GPP 78 is a potent inhibitor of Nampt (IC50 = 3 nM). It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy. | [Uses]
GPP78 (CAY10618) is a potent Nampt inhibitor with an IC50 of 3.0 nM for nicotinamide adenine dinucleotide (NAD) depletion. GPP78 is cytotoxic to neuroblastoma cell line SH-SY5Y cells with an IC50 of 3.8 nM by inducing autophagy. GPP78 has anti-cancer and anti-inflammatory effects[1][2]. | [Definition]
ChEBI: N-(2-phenylphenyl)-8-[4-(3-pyridinyl)-1-triazolyl]octanamide is a member of biphenyls. | [in vivo]
GPP78 (10 mg/kg; intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days; male adult CD1 mice) treatment reduces the severity of spinal cord trauma in SCI mice[2]. | Animal Model: | Male adult CD1 mice (25-30 g) with spinal cord injury (SCI)[2] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; daily; 1 hour or 6 hours after SCI; for 19 days | | Result: | Significantly reduced the demyelination associated with SCI. And significantly ameliorated the functional deficits induced by SCI.
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| [References]
[1] Colombano G, et al. A novel potent nicotinamide phosphoribosyltransferase inhibitor synthesized via click chemistry. J Med Chem. 2010 Jan 28;53(2):616-23. DOI:10.1021/jm9010669
[2] Esposito E, et al. The NAMPT inhibitor FK866 reverts the damage in spinal cord injury. J Neuroinflammation. 2012 Apr 10;9:66. DOI:10.1186/1742-2094-9-66 |
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