Bay 36-7620
目录号 : GC10141
Selective mGlu1 receptor non-competitive antagonist
Cas No.:232605-26-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Metabotropic glutamate (mGlu) receptors are G proteincoupled receptors (GPCRs) that act predominantly as modulators of synaptic transmission. As such, they play a role in many physiological and pathophysiological processes. BAY36-7620 is a pPotent non-competitive mGlu1 receptor antagonist with.
In vitro: BAY36-7620 is a potent and selective antagonist at mGlu1receptors and inhibits >60% of mGlu1a receptor constitutive activity (IC50 = 0.38 μM). BAY36-7620 is thus the first described mGlu1 receptor inverse agonist. Moreover, BAY36-7620 did not displace the [3H]quisqualate binding from the Glu-binding pocket, indicating that BAY36-7620 is a noncompetitive mGlu1 antagonist [2].
In vivo: BAY 36-7620 protected against pentylenetetrazole-induced convulsions in the mouse. As assessed in rats, BAY 36-7620 was devoid of the typical side effects of the ionotropic glutamate (iGlu) receptor antagonists phencyclidine and MK-801. Therefore, BAY 36-7620 did not disrupt sensorimotor gating, induce phencyclidine-like discriminative effects or stereotypical behavior, or facilitate intracranial self-stimulated behavior [3].
Clinical trial: Up to now, BAY 36-7620 is still in the preclinical development stage.
Reference:
[1] Carroll FY, Stolle A, Beart PM, Voerste A, Brabet I, Mauler F, Joly C, Antonicek H, Bockaert J, Müller T, Pin JP, Prézeau L. BAY36-7620: a potent non-competitive mGlu1 receptor antagonist with inverse agonist activity. Mol Pharmacol. 2001 May;59(5):965-73.
[2] De Vry J, Horváth E, Schreiber R. Neuroprotective and behavioral effects of the selective metabotropic glutamate mGlu(1) receptor antagonist BAY 36-7620. Eur J Pharmacol. 2001 Oct 5;428(2):203-14.
| Cas No. | 232605-26-4 | SDF | |
| 化学名 | (3aS,6aS)-5-methylene-6a-(naphthalen-2-ylmethyl)hexahydro-1H-cyclopenta[c]furan-1-one | ||
| Canonical SMILES | O=C1OC[C@@H](C2)[C@](CC3=CC=C4C(C=CC=C4)=C3)1CC2=C | ||
| 分子式 | C19H18O2 | 分子量 | 278.35 |
| 溶解度 | <27.84mg/ml in ethanol; <27.84mg/ml in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5926 mL | 17.963 mL | 35.926 mL |
| 5 mM | 0.7185 mL | 3.5926 mL | 7.1852 mL |
| 10 mM | 0.3593 mL | 1.7963 mL | 3.5926 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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