ST3932
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.
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- CAS 番号: 1246018-21-2
- 分子式: C12H16N8O
- 分子量:288.31
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Adenosine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
Ki: 8 nM (A2A receptor), 33 nM (A1 receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
450 nM
Compound: 16a, (R,S)-16a
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Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
Antagonist activity at human adenosine A2A receptor expressed in HEK293 cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 10 mins prior to NECA addition
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[PMID: 23789814] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1246018-21-2
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分子量 288.31
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分子式 C12H16N8O
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SMILES
OC(C)CCC1=NC(N(C)C(N2N=CC=N2)=N3)=C3C(N)=N1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)