2. Metabolic Enzyme/Protease
  3. DAGL
  4. A1480LS

A1480LS 是一种外周限制性、口服有效的 DAGLα 和 DAGLβ 的共价且不可逆抑制剂，在人源靶点中的 IC50 值分别为 6 nM 和 4 nM，在小鼠、大鼠、犬、猴和人源体系中的 IC50 均 ≤15 nM。A1480LS 可降低 2-花生四烯酸甘油酯、花生四烯酸以及环氧合酶和脂氧合酶衍生的类二十烷酸水平。A1480LS 可抑制外周坐骨神经中由损伤诱导的 2-花生四烯酸甘油酯和花生四烯酸的生成，并抑制高阈值和宽动态范围样背角神经元对机械刺激的反应。A1480LS 可减轻炎症性疼痛、神经性疼痛和化疗诱导的周围神经病大鼠模型的疼痛行为。

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A1480LS

A1480LS Chemical Structure

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A1480LS 相关抗体

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DAGLα DAGLβ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

A1480LS is a peripherally restricted, orally effective covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy[1].

IC50 & Target

DAGLα

 

DAGLβ

 

体内研究
(In Vivo)

A1480LS (1-20 mg/kg; p.o.; 2 次) 可通过抑制外周 DAGL 且不改变脑内 2-AG 水平，在大鼠 CFA 炎性疼痛模型中呈剂量依赖性缓解机械性痛觉过敏，其 ED50 为 7.7 mg/kg[1]。
A1480LS (15, 20 mg/kg; p.o.) 可在连续给药 5 天的过程中，快速缓解并持续抑制大鼠由紫杉醇诱导的机械性痛觉过敏；还可逆转并维持大鼠由 CCI 诱导的机械性异常痛觉至假手术水平，同时可将坐骨神经中由损伤诱导的 2-AG 及 AA 水平升高恢复至正常状态，但不会影响大脑中这些脂质的水平[1]。
A1480LS (1 mg/kg; i.v.) 可在麻醉 CCI 大鼠中选择性抑制 HT 和类 WDR 背角神经元的活动，且不改变 LTMR 的活动，这表明其可抑制脊髓伤害性感觉输入[1]。
A1480LS (8-30 mg/kg; p.o.) 不会调节大鼠中 PTZ 诱导的癫痫发作敏感性或脑内 2-AG 水平，且在 Rattus norvegicus 大鼠中耐受性良好，仅在部分动物中观察到轻微、短暂的腹部肌张力降低；说明其无中枢神经系统致痫风险[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague Dawley (male, 176-206 g, intraplantar CFA injection)[1]
Dosage: 1 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: p.o.; 2 doses (2 h before CFA, 24 h after CFA)
Result: Increased mechanical withdrawal thresholds dose-dependently 4 h after the second dose, with an ED50 of 7.7 mg/kg.
Achieved average blood concentrations of 1.1 μM (free plasma concentrations=1.5 nM) at 20 mg/kg, with an EC50 of 0.22 μM to suppress allodynia.
Inhibited kidney DAGLβ activity and reduced kidney 2-AG concentrations dose-dependently.
Caused partial brain DAGLα/β inhibition at 10 and 20 mg/kg without brain 2-AG depletion.
Animal Model: Sprague Dawley (male, intraperitoneal paclitaxel injection 1 mg/kg daily for 5 consecutive days)[1]
Dosage: 15 mg/kg (single dose; established allodynia); 15 mg/kg (repeated dosing; maintained anti-allodynic effects)
Administration: p.o.; single dose on day 7; once daily for 5 days (days 15-18)
Result: Attenuated established mechanical allodynia 4 h post-dose on day 7 with a single 15 mg/kg oral dose.
Maintained significant anti-allodynic effects over 5 days with repeated once-daily dosing of 15 mg/kg from days 15-18, comparable to duloxetine.
Animal Model: Sprague Dawley (male, 200-220 g at surgery; 233-289 g at dosing, chronic constriction injury of left common sciatic nerve)[1]
Dosage: 20 mg/kg (repeated dosing; allodynia reversal); 20 mg/kg (single dose; lipid analysis)
Administration: p.o.; once daily for 5 days (days 14-18); single dose 14 days post-CCI
Result: Reversed allodynia and restored von Frey thresholds to sham levels with repeated 20 mg/kg dosing, with efficacy comparable to naproxen and pregabalin.
Reduced 2-AG and normalized AA concentrations in injured sciatic nerves with a single 20 mg/kg dose, after CCI caused a 7-fold increase in 2-AG and 2-fold increase in AA.
Animal Model: Sprague Dawley (male, 250-315 g, chronic constriction injury of left sciatic nerve, right jugular vein catheter implantation)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
Administration: i.v.; single bolus after baseline vehicle recording
Result: Produced dose-dependent modulation of high-threshold (HT) and wide dynamic range-like (WDR-like) single-unit responses, with robust suppression at 1 mg/kg.
Did not modulate low-threshold mechanoreceptor (LTMR) single-unit activity at 1 mg/kg.
Animal Model: Sprague Dawley (male, 208-263 g, subcutaneous pentylenetetrazole injection 80 mg/kg)[1]
Dosage: 8 mg/kg; 16 mg/kg; 30 mg/kg
Administration: p.o.; single dose 4 h pre-PTZ
Result: Did not alter convulsion latency or occurrence at any tested dose.
Did not change brain 2-AG levels following administration.
分子量

542.55

Formula

C30H25F3N6O
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

A1480LS 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A1480LSDAGLDiacylglycerol lipaseDAG lipaseDGLsciatic nervesDAGLαDAGLβarachidonic acidneuropathic paincyclooxygenaselipoxygenase2-arachidonoylglyceroldorsal horn neuroninflammatory painInhibitorinhibitorinhibit

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A1480LS
目录号：
HY-181482
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