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ST3932 Sale

目录号 : GC31197

ST3932是ST1535的代谢物,为adenosineA2A受体拮抗剂,对A2A和A1受体的Ki值分别为8nM和33nM。

ST3932 Chemical Structure

Cas No.:1246018-21-2

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Animal experiment:

Mice[1]Catalepsy is induced by haloperidol (2 mg/kg) injected intraperitoneally (i.p.) 2.5 h before oral administration of 10, 20, and 40 mg/kg ST1535, ST3932, ST4206 or vehicle. An additional group without haloperidol (control group) with only vehicle is administered. At time 0 min, successful induction of catalepsy in all animals is checked before compounds administration, then, catalepsy is scored every 60 min for 3 h. Each mouse is gently placed by its forepaws on a wire at a height of 4.5 cm. The catalepsy is measured as the time necessary for the animal to step down with at least one forepaw with a cut off time for each animal of 60 s; after this time the mouse is gently removed from the wire. Catalepsy is recorded using a video-camera and by an observer who is unaware of the treatment[1].Rats[1]Two weeks after the unilateral 6-OHDA-lesion, rats are screened on the basis of their contralateral rotation in response to l-DOPA (50 mg/kg i.p.)+benserazide (30 mg/kg i.p.). Rats not showing at least 200 contralateral rotations during 3 h testing period are eliminated from the study. One week later, rats are administered with the threshold dose of l-DOPA (3 mg/kg i.p.)+benserazide (6 mg/kg i.p.) in combination with vehicle (10% sucrose and 0.3% Tween 80 in sterile water i.p.) or with ST1535, ST3932 and ST4206 respectively (10, 20 and 40 mg/kg i.p.). l-DOPA is administered 5 min after vehicle or molecules in study, whereas benserazide is administered 30 min before l-DOPA injection. Contralateral rotations are measured every 10 min for 2 h by Rotameter system[1].

References:

[1]. ST3932, et al. Animal models of Parkinson׳s disease: Effects of two adenosine A2A receptor antagonists ST4206 and ST3932, metabolites of 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535). Eur J Pharmacol. 2015 Aug 15;761:353-61.

产品描述

ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.

ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively. ST3932 inhibits agonist-induced cAMP accumulation with an IC50 value of 450 nM[1].

ST3932 (10, 20, 40 mg/kg, p.o.) antagonizes haloperidol-induced catalepsy, and increases motor activity in mice. ST3932 (20, 40 mg/kg, i.p.) significantly increases the number of contralateral turns induced by l-DOPA in rats[1].

[1]. ST3932, et al. Animal models of Parkinson?s disease: Effects of two adenosine A2A receptor antagonists ST4206 and ST3932, metabolites of 2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535). Eur J Pharmacol. 2015 Aug 15;761:353-61.

Chemical Properties

Cas No. 1246018-21-2 SDF
Canonical SMILES OC(C)CCC1=NC(N(C)C(N2N=CC=N2)=N3)=C3C(N)=N1
分子式 C12H16N8O 分子量 288.31
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 3.4685 mL 17.3424 mL 34.6849 mL
5 mM 0.6937 mL 3.4685 mL 6.937 mL
10 mM 0.3468 mL 1.7342 mL 3.4685 mL
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