2. GPCR/G Protein
  3. Adenosine Receptor
  4. PSB 0777 ammonium

PSB 0777 ammonium 是一种有效的选择性腺苷 A2A 受体激动剂，对大鼠和人 A2A 受体的 Ki 值分别为 44.4 nM，360 nM。PSB 0777 ammonium 对大鼠和人的 A1 受体的 Ki 值分别 ≥10000 nM，541 nM。PSB 0777 ammonium 显示出较差的大脑渗透性和口服生物利用度。PSB 0777 ammonium 具有用于炎性肠病 (IBS) 研究的潜力。

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PSB 0777 ammonium Chemical Structure

PSB 0777 ammonium Chemical Structure

CAS No. : 2122196-16-9

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Other Forms of PSB 0777 ammonium:

PSB 0777 ammonium 相关抗体

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查看 Adenosine Receptor 亚型特异性产品:

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research[1][2][3].

IC50 & Target

Ki: 44.4 nM (rat A2A), 360 nM (human A2A), ≥10000 nM (rat A1) and 541 nM (human A1)[1]
体外研究
(In Vitro)

PSB 0777 ammonium (compound 7) shows high selectivity for the A2AAR (>225-fold) versus the other AR subtypes (Ki values of >10000 nM and 10000 for human A2B receptor and A3 receptor, respectively). PSB 0777 ammonium acts as an full agonist at A2AAR with an EC50 value of 117 nM in CHO-K1 cells[1].
PSB-0777 ammonium binds human β1 (Ki=4.4 μM) and β3 (Ki=3.3 μM) adrenergic receptors[2].
PSB 0777 ammonium (0.1 μM, 1 μM, 10 μM) increases concentration-dependently Acetylcholine (Ach, 1 mM) contractions in untreated and inflamed rat ileum/jejunum preparations in ex vivo experiments[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PSB 0777 ammonium 相关抗体:
体内研究
(In Vivo)

PSB 0777 ammonium (0.4 mg/kg/day; oral gavage; from the day 5 to 10) causes a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture[3].
PSB 0777 ammonium (0.03, 0.3, 3 mg/kg; i.p.) causes dose-dependent hypothermia and hypoactivity in C57BL/6J mice[2].
PSB 0777 ammonium cannot be absorbed systemically by the digestive mucosa once administered by the oral route. PSB 0777 ammonium (0.4 mg/kg/day; PO) has very low plasma concentrations in rats at 30 min (below 5 nM), and there is no plasma concentrations at 60 min after administration. PSB 0777 ammonium (0.4 mg/kg/day; IP) makes plasma concentrations well evident at 30 min, and decreases after 60 min, and is not detectable at 120 and 240 min[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Albino male Sprague-Dawley rats of 200 g with Oxazolone-induced colitis[3]
Dosage: 0.4 mg/kg
Administration: Oral gavage; daily; from the day 5 to 10
Result: Caused a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture alone or in combination with Dexamethasone (1 mg/kg/day).
Counteracted significantly the increment of colonic myeloperoxidase (MPO) levels associated with colitis.
分子量

500.55

Formula

C18H24N6O7S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

PSB 0777 ammonium 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PSB 07772122196-16-9PSB0777PSB-0777Adenosine ReceptorP1 receptorA2AA1brainpenetrantinflammatoryboweldiseaseIBSA2BA3β1β3AcetylcholineInhibitorinhibitorinhibit

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产品名称：
PSB 0777 ammonium
目录号：
HY-136233
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