中文名稱(chēng):DOTA.SA.FAPI | 英文名稱(chēng):DOTA.SA.FAPI |
品牌: TanzhenBio | 產(chǎn)地: 江西 |
保存條件: -20℃ | 純度規(guī)格: 98% |
產(chǎn)品類(lèi)別: 放射顯影多肽產(chǎn)品 | |
是否進(jìn)口: 否 |
Recently, the first squaramide-(SA) containing FAP inhibitor-derived radiotracers were introduced. DATA5m.SA.FAPi and DOTA.SA.FAPi with their non-radioactive complexes showed high affinity and selectivity for FAP. After a successful preclinical study with [68Ga]Ga-DOTA.SA.FAPi, the first patient studies were realized for both compounds. Here, we present a new squaramide-containing compound targeting FAP, based on the AAZTA5 chelator 1,4-bis-(carboxylmethyl)-6-[bis-(carboxymethyl)-amino-6-pentanoic-acid]-perhydro-1,4-diazepine. For this molecule (AAZTA5.SA.FAPi), complexation with radionuclides such as gallium-68, scandium-44, and lutetium-177 was investigated, and the in vitro properties of the complexes were characterized and compared with those of DOTA.SA.FAPi. AAZTA5.SA.FAPi and its derivatives labelled with non-radioactive isotopes demonstrated similar excellent inhibitory potencies compared to the previously published SA.FAPi ligands, i.e., sub-nanomolar IC50 values for FAP and high selectivity indices over the serine proteases PREP and DPPs. Labeling with all three radiometals was easier and faster with AAZTA5.SA.FAPi compared to the corresponding DOTA analogue at ambient temperature. Especially, scandium-44 labeling with the AAZTA derivative resulted in higher specific activities. Both DOTA.SA.FAPi and AAZTA5.SA.FAPi showed sufficiently high stability in different media. Therefore, these FAP inhibitor agents could be promising for theranostic approaches targeting FAP.
成立日期 | 2019-02-05 (7年) | 注冊(cè)資本 | 300萬(wàn)人民幣 |
員工人數(shù) | 10-50人 | 年?duì)I業(yè)額 | ¥ 100萬(wàn)-300萬(wàn) |
主營(yíng)行業(yè) | 生物活性小分子,有機(jī)合成試劑,氨基糖苷類(lèi) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠(chǎng),試劑,定制,服務(wù) |