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NAV-2729
产品别名
419547-11-8
NAV-2729
NAV 2729
3-(4-Chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)-pyrazolo[1,5-a]pyrimidin-7(4H)-one
NAV2729
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C25H17ClN4O3 |
| Molecular weight | 456.88 |
| MDL number | MFCD01455625 |
| NACRES | NA.77 |
| Biochem/physiol Actions【生化/生理作用】 | 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) that targets ARF6 GEF-binding region, NAV-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 xenograft mice in vivo (30 mg/kg/day i.p.). NAV-2729 (IC50 of 1.5 μM) has a therapeutic benefit in reducing the adverse effect of diabetic retinopathy in animal models. |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | O=C1C=C(C2=CC=C([N+]([O-])=O)C=C2)NC3=C(C4=CC=C(Cl)C=C4)C(CC5=CC=CC=C5)=NN31 |
安全信息
| Storage Class Code【储存分类代码】 | 13 - Non Combustible Solids |
| WGK | WGK 3 |
