S87943 |
ST034307 |
源葉(MedMol) | 98% |
- 產品描述: 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:
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
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質量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)