Product Name :
NAV-2729
Description:
NAV-2729 is a dual Arf1/Arf6 activation inhibitor.
CAS:
419547-11-8
Molecular Weight:
456.88
Formula:
C25H17ClN4O3
Chemical Name:
2-benzyl-3-(4-chlorophenyl)-5-(4-nitrophenyl)-1H,7H-pyrazolo[1,5-a]pyrimidin-7-one
Smiles :
[O-][N+](=O)C1C=CC(=CC=1)C1=CC(=O)N2NC(CC3C=CC=CC=3)=C(C2=N1)C1C=CC(Cl)=CC=1
InChiKey:
WHYGBVWGARJOCS-UHFFFAOYSA-N
InChi :
InChI=1S/C25H17ClN4O3/c26-19-10-6-18(7-11-19)24-22(14-16-4-2-1-3-5-16)28-29-23(31)15-21(27-25(24)29)17-8-12-20(13-9-17)30(32)33/h1-13,15,28H,14H2
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
NAV-2729 is a dual Arf1/Arf6 activation inhibitor.|Product information|CAS Number: 419547-11-8|Molecular Weight: 456.88|Formula: C25H17ClN4O3|Chemical Name: 2-benzyl-3-(4-chlorophenyl)-5-(4-nitrophenyl)-1H,7H-pyrazolo[1,5-a]pyrimidin-7-one|Smiles: [O-][N+](=O)C1C=CC(=CC=1)C1=CC(=O)N2NC(CC3C=CC=CC=3)=C(C2=N1)C1C=CC(Cl)=CC=1|InChiKey: WHYGBVWGARJOCS-UHFFFAOYSA-N|InChi: InChI=1S/C25H17ClN4O3/c26-19-10-6-18(7-11-19)24-22(14-16-4-2-1-3-5-16)28-29-23(31)15-21(27-25(24)29)17-8-12-20(13-9-17)30(32)33/h1-13,15,28H,14H2|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 50 mg/mL (109.{{Fexinidazole} web|{Fexinidazole} Parasite|{Fexinidazole} Protocol|{Fexinidazole} Description|{Fexinidazole} manufacturer|{Fexinidazole} Epigenetics} 44 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.{{Mirogabalin} web|{Mirogabalin} Neuronal Signaling|{Mirogabalin} Purity & Documentation|{Mirogabalin} Data Sheet|{Mirogabalin} supplier|{Mirogabalin} Epigenetics} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|NAV-2729 directly binds to Arf6. Based on a structural homology model of the Arf6/Arf6-GEF complex, it is predicted that NAV-2729 associates with Arf6 at the Arf6 GEF-binding area, which is distinct from the guanine nucleotide-binding pocket of Arf6.PMID:28322188 NAV-2729 blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell. NAV-2729 is a dual Arf1/Arf6 inhibitor and is more effective toward Arf1 than Arf6. NAV-2729 blocks spontaneous activation of Arf6 and its activation by cytohesins and BRAG. NAV-2729 is an inhibitor of the spontaneous activation of Arf6, and it also inhibits the activation of Arf6 by its GEFs, ARNO and BRAG2, in solution. The inhibitory profile of NAV-2729 is analyzed at a concentration of 25 μM, which is reported to result in almost total inhibition of spontaneous and GEF-stimulated Arf6 activation in vitro. Under the conditions used in assays, NAV-2729 inhibits spontaneous nucleotide exchange of Δ13Arf6 by ~15%. NAV-2729 inhibits the activation of Δ13Arf6 by BRAG2Sec7PH by 25%. Δ17Arf1 has no measurable spontaneous nucleotide exchange. Activation of Δ17Arf1 by BRAG2Sec7PH is inhibited by NAV-2729, and the efficiency is markedly higher than that for Arf6 (50%). In a dose-response experiment, nucleotide exchange rates are reduced by 50% by 10 μM NAV-2729 for Δ17Arf1 while 50% inhibition is not achieved even at 25 μM NAV-2729 for Δ13Arf6.|In Vivo:|Systemic treatment of mice with NAV-2729 interfere with tumorigenesis and tumor growth in orthotopic xenograft mouse model of uveal melanoma.|Products are for research use only. Not for human use.|