產(chǎn)品描述: | ST034307 is a potent and selective adenylyl cyclase 1 (AC1) inhibitor, with IC50 of 2.3 μM. |
靶點: |
IC50: 2.3 μM (AC1);Adenylylcyclase |
體外研究: |
ST034307 reveals selective inhibition of AC1 and potentiates AC8 activity to a nonsignificant small extent. ST034307 potentiates phorbol 12-myristate 13-acetate (PMA)-stimulated cAMP production by AC2. ST034307 significantly inhibits the forskolin- or isoproterenol-stimulated AC1 activity in HEK cells stably expressing AC1. In contrast, ST034307 has no significant effects in the wild-type HEK cells. ST034307 significantly inhibits the Ca2+/calmodulin-stimulated cAMP accumulation in the hippocampal homogenates. ST034307 dose-dependently inhibits both the development and the maintenance of MOR-mediated sensitization of AC1。 |
體內(nèi)研究: |
ST034307 (0.25 μg) causes a significant relief of CFA-induced inflammatory pain in mice. ST034307 exhibits an estimated median effective dose (E50) value for analgesia of 0.28 μg in the mouse pain model。 |
參考文獻(xiàn): |
1. Brust TF, Alongkronrusmee D, Soto-Velasquez M, Baldwin TA, Ye Z, Dai M, Dessauer CW, van Rijn RM, Watts VJ. Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties. Sci Signal. 2017 Feb 21;10(467). pii: eaah5381. doi: 10.1126/scisignal.aah5381. PubMed PMID: 28223412. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
3.356 ml |
16.781 ml |
33.563 ml |
5 mM |
0.671 ml |
3.356 ml |
6.713 ml |
10 mM |
0.336 ml |
1.678 ml |
3.356 ml |
50 mM |
0.067 ml |
0.336 ml |
0.671 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |