| Identification | Back Directory | [Name]
NAV2729 | [CAS]
419547-11-8 | [Synonyms]
NAV2729
CS-2790
Grassofermata
NAV-2729;NAV2729
NAV-2729 >=98% (HPLC)
Grassofermata，NAV2729
2-Benzyl-3-(4-chlorophenyl)-5-(4-nitrophenyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one
3-(4-Chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one
Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 3-(4-chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)- | [Molecular Formula]
C25H17ClN4O3 | [MDL Number]
MFCD01455625 | [MOL File]
419547-11-8.mol | [Molecular Weight]
456.88 |
| Chemical Properties | Back Directory | [Boiling point ]
678.0±65.0 °C(Predicted) | [density ]
1.40±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 2 mg/ml | [form ]
A crystalline solid | [pka]
-2.43±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
NAV 2729 is a selective ARF6 inhibitor. | [Definition]
ChEBI:NAV2729 is a pyrazolopyrimidine that is 4H-pyrazolo[1,5-a]pyrimidin-7-one which is substituted at positions 2, 3, and 5 by benzyl, p-chlorophenyl, and p-nitrophenyl groups, respectively. It is an inhibitor of ADP-ribosylation factor 6 (ARF6), a member of the ADP ribosylation factor family of GTP-binding proteins. It has a role as an inhibitor. It is a pyrazolopyrimidine, a C-nitro compound and a member of monochlorobenzenes. | [Biological Activity]
NAV-2729 (IC50 of\u20091.5\u2009μM) has a therapeutic benefit in reducing the adverse effect of diabetic retinopathy in animal models.''Originally characterized as a non-nucleotide-competitive and reversible ARF6-selective inhibitor (IC50 = 1.4 μM without GEF and 2.4 μM with 100 nM ARNO or BRAG2/GEP100) th at targets ARF6 GEF-binding regionNAV-2729 prevents GEF-dependent ARF1 & ARF6 activity (% inhibition of BRAG2Sec7PH-stimulated GTPase activity/[NAV-2729] = 50% Δ17Arf1/10 μM and 15% Δ13Arf6/25 μM) with higher potency against BRAG2- than ARNO-dependent ARF1 activity (64% vs. 20% Δ17Arf1 inhibition at 25 μM in the presence of respective GEF sec7 domain). NAV-2729 treatment effectively inhibits G-alpha-q downstream signaling pathways and anchorage-independent colony growth of Mel92.1 & Mel202 melanoma cells in vitro (10 μM) as well as uveal melanoma tumor establishment in Mel202 x | [in vivo]
Systemic treatment of mice with NAV-2729 interfere with tumorigenesis and tumor growth in orthotopic xenograft mouse model of uveal melanoma[1]. | [storage]
Store at -20°C |
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