产品介绍
Product Description
Biochem/physiol Actions
PF-06928215 is a high affinity (KD of the (1R,2S) enantiomer = 200 nM) active site-targeting, substrate-competitive cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 4.9 μM using the (1R,2S) enantiomer; in the presence of 1 mM ATP, 0.3 mM GTP, 100 nM 45-bp interferon-stimulatory dsDNA (ISD)). PF-06928215 displays no inhibitory potency against dsDNA-induced IFN-β expression in cellular cGAS assays, most likely due to limited cell-permeability and/or high levels of cellular ATP and GTP in the reporter cells employed. Note: this product contains the two cis-enantiomers (1R,2S) and (1S,2R).
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear (Warmed) |
| storage temp. | 2-8°C |
| SMILES string | OC([C@H](CCCC1)[C@H]1NC(C2=C3N(N=C2)C(C=C(C4=CC=CC=C4)N3)=O)=O)=O |
| InChI | 1S/C20H20N4O4/c25-17-10-16(12-6-2-1-3-7-12)22-18-14(11-21-24(17)18)19(26)23-15-9-5-4-8-13(15)20(27)28/h1-3,6-7,10-11,13,15,22H,4-5,8-9H2,(H,23,26)(H,27,28)/t13-,15+/m1/s1 |
| InChI key | LCOWXYIOVWEZPJ-HIFRSBDPSA-N |
