L-Palmitoylcarnitine
(Synonyms: 棕榈酰肉碱) 目录号 : GC30745
L-Palmitoylcarnitine 是一种重要的内源性脂肪酸代谢物，可同时提高离子通道对 ATP 的敏感性，IC50 值在 30.3 ± 5.5µM和62.0 ± 2.7之间。
Cas No.:2364-67-2
Sample solution is provided at 25 µL, 10mM.
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L-Palmitoylcarnitine is an important endogenous fatty acid metabolite that simultaneously enhanced the ATP sensitivity of the ion channel with IC50 value fell from 62.0 ± 2.7 to 30.3 ±5.5µM[1]. L-Palmitoylcarnitine is a critical regulator in fatty acids metabolism, especially in mitochondrial fatty acid β-oxidation[2]. L-Palmitoylcarnitine weakly inhibits pyruvate-supported respiration in mitochondria but does not affect pyruvate utilization. It has stronger inhibitory effect on acetylcarnitine oxidation[3].
In vitro, L-Palmitoylcarnitine (1–10μM) incubated guinea-pig ventricular myocytes at 35°C for 10min largely inhibited the outward current transient associated with Na/K pump current[4]. L-Palmitoylcarnitine (10nM to10μM) incubated isolated guinea-pig ventricular myocytes for 40min produced concentration- and time-dependent changes of resting potential (RP) and action potential duration at 50% repolarization (APD50)[5].
In vivo, L-Palmitoylcarnitine (0, 0.25, 1, 4mg/kg) administrated into FeCl3-induced mouse thrombosis model and transient middle cerebral artery occlusion (tMCAO) mouse models via tail vein injections significantly inhibited FeCl3-induced arterial thrombosis, and also mitigated intracerebral thrombosis and inflammation in a transient middle cerebral artery occlusion (tMCAO) mouse model[6].
References:
[1] Haruna T, Horie M,Takano M,et al. Alteration of the membrane lipid environment by L-palmitoylcarnitine modulates K(ATP) channels in guinea-pig ventricular myocytes. Pflugers Arch. 2000;441(2-3):200-207.
[2] Liu Q Y, Li P W, Ma J L, et al. Arsenic exposure at environmentally relevant levels induced metabolic toxicity in development mice: Mechanistic insights from integrated transcriptome and metabolome. Environ Int. 2024 Aug:190:108819.
[3] Hutson S M, van Dop C, Lardy H A. Metabolism of pyruvate and carnitine esters in bovine epididymal sperm mitochondria. Arch Biochem Biophys. 1977 May;181(1):345-52.
[4] Tanaka M, Gilbert J, Pappano A J. Inhibition of sodium pump by l-palmitoylcarnitine in single guinea-pig ventricular myocytes. J Mol Cell Cardiol. 1992 Jul;24(7):711-9.
[5] Mészàros J, Pappano A J. Electrophysiological effects of L-palmitoylcarnitine in single ventricular myocytes. Am J Physiol. 1990 Apr;258(4 Pt 2):H931-8.
[6] Yang J, Cha L, Wang Y P, et al. L-Palmitoylcarnitine potentiates plasmin and tPA to inhibit thrombosis. Nat Prod Bioprospect. 2023 Nov 8;13(1):48.
L-Palmitoylcarnitine 是一种重要的内源性脂肪酸代谢物，可同时提高离子通道对 ATP 的敏感性，IC50 值在 30.3 ± 5.5µM和62.0 ± 2.7之间[1]。L-Palmitoylcarnitine 是脂肪酸代谢，尤其是线粒体脂肪酸 β-氧化的关键调控因子[2]。L-Palmitoylcarnitine 对丙酮酸支持的线粒体呼吸仅呈弱抑制，但不影响丙酮酸本身的利用，而对乙酰肉碱氧化的抑制作用更强[3]。
在体外实验中，L-Palmitoylcarnitine (1–10μM) 于35°C孵育豚鼠心室肌细胞10min，几乎完全抑制Na/K泵电流相关的外向瞬时电流[4]。L-Palmitoylcarnitine (10nM至10μM) 孵育离体豚鼠心室肌细胞40min，呈浓度-和时间依赖性改变静息电位及50%复极动作电位时程 (APD50)[5]。
在体内实验中，L-Palmitoylcarnitine (0、0.25、1、4mg/kg) 经尾静脉注射给予FeCl3诱导的小鼠血栓模型及短暂大脑中动脉阻塞 (tMCAO) 小鼠模型，显著抑制FeCl3诱导的动脉血栓形成，并在tMCAO模型中减轻脑内血栓与炎症[6]。
| Kinase experiment [1]: | |
Preparation Method | The enzymatic reactions were conducted in 50mM Tris–HCl buffer (pH 7.8) at 37 °C. Initially, the proteases, plasmin (30nM) and tPA (20nM), and serial dilutions of L-Palmitoylcarnitine (6.25–100μM) were incubated in buffer at 37°C for 5min, followed by the addition of their corresponding chromogenic substrates, CS-41 (0.2mM) for plasmin and CS-05 (0.2mM) for tPA, to initiate the reaction. The rate of substrate hydrolysis was monitored continuously at 405nm. |
Reaction Conditions | 6.25–100μM; 5min |
Applications | L-Palmitoylcarnitine enhanced the abilities of plasmin and tPA to hydrolyze their chromogenic substrates.L-Palmitoylcarnitine could directly bind to two enzymes (plasmin and tPA) that are responsible for thrombolysis and fibrin(ogen)olysis. Through high-affinity interactions with plasmin (KD=6.47nM) and tPA (KD=4.46nM). |
| Cell experiment [2]: | |
Cell lines | Guinea-pig ventricular myocytes |
Preparation Method | Guinea-pig ventricular myocytes were incubated with L-Palmitoylcarnitine (1–10μM) at 35°C for 10min. |
Reaction Conditions | 1–10μM; 10min |
Applications | L-Palmitoylcarnitine largely inhibited the outward current transient associated with Na/K pump current. |
| Animal experiment [3]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | FeCl3-induced mouse thrombosis model and transient middle cerebral artery occlusion (tMCAO) mouse models were treated with L-Palmitoylcarnitine (0, 0.25, 1, 4mg/kg) administered via tail vein injections. |
Dosage form | 0, 0.25, 1, 4mg/kg; i.v.; a single administration |
Applications | L-Palmitoylcarnitine administration significantly inhibited FeCl3-induced arterial thrombosis. It also mitigated intracerebral thrombosis and inflammation in a transient middle cerebral artery occlusion (tMCAO) mouse model. |
References: | |
| Cas No. | 2364-67-2 | SDF | |
| 别名 | 棕榈酰肉碱 | ||
| Canonical SMILES | CCCCCCCCCCCCCCCC(O[C@H](CC([O-])=O)C[N+](C)(C)C)=O | ||
| 分子式 | C23H45NO4 | 分子量 | 399.61 |
| 溶解度 | Ethanol : 25 mg/mL (Need ultrasound) | 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 | 2.5024 mL | 12.5122 mL | 25.0244 mL |
| 5 mM | 500.5 μL | 2.5024 mL | 5.0049 mL |
| 10 mM | 250.2 μL | 1.2512 mL | 2.5024 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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Quality Control & SDS
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- Purity: >97.00%
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