MDL 12330A hydrochloride
(Synonyms: RMI 12330A) 目录号 : GC12075An adenylyl cyclase inhibitor
Cas No.:40297-09-4
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
IC50: 1.5 X 10-5 M for histamine-stimulated adenylate cyclase [1].
RMI 12330 A is N,-(cis-2-phenylcyclopentyl) azacyclotridecan-2-imine hydrochloride, which has been reported to inhibit choleratoxin-induced intestinal hypersecretion, presumably via an inhibition of mucosal adenylate cyclase.
In vitro: RMI 12330 A at the concentration of ranging from 10 uM to 5 mM the can effectively inhibit the adenylate cyclase activity of a rat liver plasma membrane preparation. RMI 12330 A does not apply its competition on the catalytic site of the enzyme to perform its inhibitory action. The inhibition activity of RMI 12330 A upon adenylate cyclase was due to an irreversible binding with the plasma membranes [2].
Ex vivo: In the isolated work-performing heart of the guinea-pig, RMI 12330A depressed all cardiac functions with the IC50 of 1.1 X 10-6 M, including contractile force, dP/dt, dF/dt, pressures developed, stroke work and work performance. The positive inotropic response to increasing heart rate (staircase) and left atrial pressure rose became negative. Ouabain, isoprenaline and histamine, no longer had positive inotropic effects. After its depression by RMI 12330A, the cardiac function can be completely restored by increasing the perfusate calcium concentration from 2.5 mm to 4.5 and 6.5 mm [1].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Grupp G, Grupp IL, Johnson CL, Matlib MA, Rouslin W, Schwartz A, Wallick ET, Wang T, Wisler P. Effects of RMI 12330A, a new inhibitor of adenylate cyclase on myocardial function and subcellular activity. Br J Pharmacol. 1980 Nov;70(3):429-42.
[2] Guellaen G, Mahu JL, Mavier P, Berthelot P, Hanoune J. RMI 12330 A, an inhibitor of adenylate cyclase in rat liver. Biochim Biophys Acta. 1977 Oct 13;484(2):465-75.
| Cas No. | 40297-09-4 | SDF | |
| 别名 | RMI 12330A | ||
| 化学名 | (E)-N-((1R,2R)-2-phenylcyclopentyl)azacyclotridec-1-en-2-amine hydrochloride | ||
| Canonical SMILES | [C@@H](CCC1)(C2=CC=CC=C2)[C@@H]1N/C3=N/CCCCCCCCCCC3.Cl | ||
| 分子式 | C23H36N2.HCl | 分子量 | 377.01 |
| 溶解度 | 1mg/ml in DMF, 1mg/ml in Ethanol | 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 | 2.6524 mL | 13.2622 mL | 26.5245 mL |
| 5 mM | 0.5305 mL | 2.6524 mL | 5.3049 mL |
| 10 mM | 0.2652 mL | 1.3262 mL | 2.6524 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。