2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. BAY 36-7620

BAY 36-7620 是有效的，非竞争性的并且有反向激动剂活性的 mGlu1 Receptor 的拮抗剂(IC50 为 0.16 μM)。BAY 36-7620 通过抑制 mGlu1 受体来抑制肿瘤生长并延长肿瘤小鼠寿命。BAY 36-7620 抑制 A549 肿瘤中的 AKT 磷酸化。BAY 36-7620 对急性硬膜下血肿大鼠模型具有神经保护作用。BAY 36-7620 可用于非小细胞肺癌和乳腺癌研究。

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BAY 36-7620 Chemical Structure

BAY 36-7620 Chemical Structure

CAS No. : 232605-26-4

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规格 价格 是否有货 数量
5 mg ￥3089
3 - 4 周
10 mg   询价  
50 mg   询价  

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BAY 36-7620 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research[1][2][3][4].

IC50 & Target

mGluR 1

0.16 μM (IC50)

mGluR1a

0.38 μM (IC50)

mGluR2

0.14 μM (IC50)

mGluR 5

0.24 μM (IC50)

体外研究
(In Vitro)

BAY 36-7620 (0.1-10 μM) 在浓度 10 μM 时完全抑制了 HEK 293 细胞中的 mGlu1 受体[1] BAY 36-7620 (0.1-10 μM，4 天) 减少了 A549 的细胞增殖和肿瘤相关蛋白表达[2]。
BAY 36-7620 (72 小时) 抑制 MCF-7, T-47D, BT-474, MDA-MB-231, Hs578T 和 BT-549 细胞生长和增殖，对他们的 IC50 分别为 27.7, 37.1, 20.8, 41.0, 21.0 和 15.7μM[3]。
BAY 36-7620 (25-50 μM，24-72 h) 引起 T-47D, BT-474, MDA-MB-231 和 BT-549 细胞 DNA 损伤并诱导了中度 G2/M 期阻滞[3]。

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

BAY 36-7620 相关抗体:

Western Blot Analysis[2]

Cell Line: A549 cell line
Concentration: 10, 25 μM
Incubation Time: Overnight
Result: Enhanced the expression of cleaved PARP and reduced bcl-2 protein expression.
Reduced the expression of HIF-1α protein and HIF activity.
Reduced the secretion of VEGF and IL-8 into supernatants.

Cell Proliferation Assay[3]

Cell Line: T MCF-7, T-47D, BT-474, MDA-MB-231, Hs578T and BT-549 cell line
Concentration: 50 μM
Incubation Time: 72 h
Result: Decreased the percentage of proliferating cells in all breast cancer cell line.
体内研究
(In Vivo)

BAY 36-7620 (5-10 mg/kg，腹腔注射；每日 1 次，连续 24 天) 抑制了胸腺裸鼠模型的肿瘤生长，延长了肺癌肿瘤小鼠的寿命[2]。
BAY 36-7620 (0.01-0.03 mg/kg，静脉注射；4 小时) 对急性硬膜下血肿大鼠模型具有神经保护作用[4]。

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

Animal Model: Lung tumors mice model[2]
Dosage: 5, 10 mg/kg
Administration: Intraperitoneal injection (i.p.); Once daily for 24 days
Result: Suppressed tumor growth in athymic mice with lung tumors.
Prolonged the survival of inoculated mice when compared to control group.
Decreased the level of AKT phosphorylation in A549 tumors.
Animal Model: Subdural hematoma rat model[4]
Dosage: 0-3 mg/kg
Administration: Intravenous injection (i.v.); 4 h
Result: Had neuroprotective effect with the efficacy of 40–50% at 0.01 and 0.03 mg/kg.
分子量

278.35

Formula

C19H18O2
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

BAY 36-7620 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

BAY 36-7620232605-26-4mGluRMetabotropic glutamate receptorsHEK 293 CellsA549 cell lineH1299 cell lineLung cancerNSCLCsBreast cancerInhibitorinhibitorinhibit

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