AC 187
目录号 : GC10097
AC 187 是一种有效且具有口服活性的胰淀素受体拮抗剂，IC50 为 0.48 nM，Ki 为 0.275 nM。
Cas No.:151804-77-2
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
Amylin is a 37-amino acid peptide co-secreted with insulin from pancreatic β-ells. The plasma concentration of amyline increases with nutrient stimuli. AC187 is a potent amylin antagonist
In vitro: AC187 potently competes for rat amylin binding at high affinity sites such as rat nucleus accumbens membranes which have been useful in developing a number of selective ligands, including AC187. The Kd for amylin at this site is 28 pM, and the Ki for AC187 is 79 pM. AC187 is relatively selective in competing for amylin binding, displacing amylin from nucleus accumbens membranes with over 400-fold greater potency [1].
In vivo: AC187 was able to inhibit metabolic responses to exogenous amylin in the intact animal. An infusion of AC187 that was itself without effect on lactate levels in anesthetized rats, inhibited by more than 90% the lactate increment evoked by infusions of rat amylin. Other experiments have shown that AC187-induced amylin blockade action is surmountable by higher doses of amylin, indicative of a competitive antagonism [1].
Clinical trial: Up to now, AC187 is still in the preclinical development stage.
Reference:
[1] Young AA, Gedulin B, Gaeta LS, Prickett KS, Beaumont K, Larson E, Rink TJ. Selective amylin antagonist suppresses rise in plasma lactate after intravenous glucose in the rat. Evidence for a metabolic role of endogenous amylin. FEBS Lett. 1994 May 2;343(3):237-41.
| Cas No. | 151804-77-2 | SDF | |
| 分子式 | C127H205N37O40 | 分子量 | 2890.25 |
| 溶解度 | Soluble to 1 mg/ml in Water | 储存条件 | Desiccate 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 | 0.346 mL | 1.73 mL | 3.4599 mL |
| 5 mM | 0.0692 mL | 0.346 mL | 0.692 mL |
| 10 mM | 0.0346 mL | 0.173 mL | 0.346 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。