|6-氯-2-(三氯甲基)-4H-苯并吡喃-4-酮|CsnPharm

CAS No.: 133406-29-8

ST034307 Catalog No. CSN20479

Synonyms: ST034307

ST034307 is an adenylyl cyclase 1 (AC1) inhibitor (IC50 = 2.3 μM), which exhibits some selectivity for AC1 over other AC isoforms.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Adenylyl Cyclase 1

IC50:2.3μM
描述ST034307 is a selective AC1 inhibitor with IC50 value of 2.3μM for inhibition of A23187-stimulated cAMP accumulation in HEK cells stably expressing AC1. Also it inhibited Ca²⁺-stimulated cAMP accumulation by AC1, as well as inhibited AC1 activity stimulated by Gas-coupled receptors in HEK-AC1 cells. It showed inhibitory activity in multiple AC1-containing membrane preparations at 100μM and mouse hippocampal homogenates at 30μM. ST034307 enhanced m-opioid receptor (MOR)–mediated inhibition of AC1 in short-term inhibition assays in HEK-AC1 cells stably transfected with MOR, with EC20 value of 0.5μM and DAMGO (4nM) and EC20 value of 7.5μM and DAMGO (15nM). However, it blocked heterologous sensitization of AC1 caused by chronic MOR activation. Intrathecal injection with 0.5μg ST034307 reduced pain responses in a mouse model of inflammatory pain. ST034307 potentiated PMA–stimulated cAMP production by AC2 and slightly potentiated forskolin-stimulated AC5 and AC6^[2].
动物研究
剂量
Rat: 3 mg/kg^[2] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rat: 3 mg/kg^[2] (i.p.)
给药途径	i.p.

[1] Brust TF, Alongkronrusmee D, et al. 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.
[2] 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):eaah5381. doi: 10.1126/scisignal.aah5381. PMID: 28223412; PMCID: PMC5734633.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.3563 mL
- 16.7814 mL
- 33.5627 mL
- 5 mM
- 0.6713 mL
- 3.3563 mL
- 6.7125 mL
- 10 mM
- 0.3356 mL
- 1.6781 mL
- 3.3563 mL

技术信息

CAS号

133406-29-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H4Cl4O2

运输

蓝冰

分子量

297.95

别名

ST034307

溶解度

DMSO	16.0 mg/mL (53.7 mM) warming

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

ST034307 Catalog No. CSN20479

靶点选择性

请登录您的专属账户

确认信息