L-692429
(Synonyms: MK-0751) 目录号 : GC60971
L-692429(MK-0751)是一种苯并内酰胺的衍生物，也是一种非肽基生长激素促分泌素(GHS)激动剂。L-692429以Ki值为63nM来结合G蛋白偶联受体(Gprotein-coupledreceptor)。
Cas No.:145455-23-8
Sample solution is provided at 25 µL, 10mM.
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L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM[1][2].
L-692429 stimulates intracellular calcium release, inositol phosphate (IP) turnover, cAMP-responsive element binding protein (CREB) activity, serum-responsive element activity and bioluminescence resonance energy transfer (BRET) activity with EC50 values of 26 nM, 47 nM, 60 nM, 63 nM and 58 nM, respectively[2].HeLa-T4 cells transiently expressing the flag epitope-tagged growth hormone secretagogue (GHS) receptor are treated with L-692429. The release of intracellular calcium is measured using fluorometry with the calcium indicator dye fluo-3/AM. Untransfected HeLa-T4 cells are unresponsive to L-692429 treatment, whereas HeLa-T4 cells transiently expressing GHS receptors demonstrate an increase in fluorescent emission after L-692429 treatment. A significant increase in luciferase activity after L-692429 treatment is seen, suggesting that activation of the GHS receptor stimulates the MAPK pathway[3].
When tested in anesthetized rats (Wistar rats), L-756867 inhibits L-692429 (100 μg/kg)-stimulated GH secretion in a dose-dependent manner. Complete inhibition is observed at an i.v. dose of 100 μg/kg of L-756867[1].
[1]. Cheng K, et al. Inhibition of L-692,429-stimulated rat growth hormone release by a weak substance P antagonist: L-756,867. J Endocrinol. 1997 Jan;152(1):155-8. [2]. Holst B, et al. Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling. Mol Endocrinol. 2005 Sep;19(9):2400-11. [3]. Cunha SR, et al. Ghrelin and growth hormone (GH) secretagogues potentiate GH-releasing hormone (GHRH)-induced cyclic adenosine 3',5'-monophosphate production in cells expressing transfected GHRH and GH secretagogue receptors. Endocrinology. 2002 Dec;143(12):4570-82.
| Cas No. | 145455-23-8 | SDF | |
| 别名 | MK-0751 | ||
| Canonical SMILES | CC(C)(N)CC(N[C@H]1C(N(CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)C5=CC=CC=C5CC1)=O)=O | ||
| 分子式 | C29H31N7O2 | 分子量 | 509.6 |
| 溶解度 | DMSO: 50 mg/mL (98.12 mM) | 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 | 1.9623 mL | 9.8116 mL | 19.6232 mL |
| 5 mM | 0.3925 mL | 1.9623 mL | 3.9246 mL |
| 10 mM | 0.1962 mL | 0.9812 mL | 1.9623 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet