A1480LS (1-20 mg/kg; orally; twice) produced dose-dependent relief of mechanoalgae hyperalgesia in a CFA-induced rat model of inflammatory pain by inhibiting peripheral DAGL without altering 2-AG levels in the brain, with an ED50 of 7.7 mg/kg [1]. A1480LS (15, 20 mg/kg; orally) rapidly relieved and sustained the inhibition of paclitaxel-induced mechanoalgae hyperalgesia in rats, remaining effective even after 5 days of continuous administration. In addition, it reversed and maintained CCI-induced mechanoalgae hyperalgesia in rats to the level of the sham-operated group, while restoring 2-AG and AA levels caused by sciatic nerve injury to normal without affecting the levels of these lipids in the brain [1]. A1480LS (1 mg/kg; intravenously) selectively inhibited the activity of HT and WDR-like neurons in the dorsal horn of the spinal cord in anesthetized CCI rats without affecting the activity of LTMRs, indicating that it inhibits spinal nociceptive input [1]. A1480LS (8-30 mg/kg; orally) did not affect pentylenetetrazole (PTZ)-induced epilepsy susceptibility or brain 2-AG levels in rats and was well tolerated in rats, with only a slight, transient decrease in abdominal muscle tone observed in some animals; these results suggest that it does not pose a risk of central nervous system-induced epilepsy [1].

Animal/Disease Models:Sprague Dawley mice (male, 176-206 g, paw-injected with CFA)[1]
Doses: 1 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
Route of Administration: Oral; Two-dose administration (2 hours before CFA injection, 24 hours after CFA injection)
Experimental Results: Four hours after the second dose, the mechanical withdrawal threshold increased in a dose-dependent manner, with an ED50 of 7.7 mg/kg. At a dose of 20 mg/kg, the mean plasma concentration reached 1.1 μM (free plasma concentration = 1.5 nM), and the EC50 for inhibiting hyperalgesia was 0.22 μM. It inhibited renal DAGLβ activity and reduced renal 2-AG concentration in a dose-dependent manner. At doses of 10 and 20 mg/kg, it caused partial inhibition of DAGLα/β in the brain, but did not lead to depletion of 2-AG in the brain.

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Animal/Disease Models:Sprague Dawley mice (male, intraperitoneal injection of paclitaxel, 1 mg/kg, once daily for 5 days)[1]
Doses: 15 mg/kg (single dose; to establish a hyperalgesia model); 15 mg/kg (repeated dose; to maintain antihyperalgesia effect)
Route of Administration: Oral; single dose on day 7; once daily for 5 days (days 15-18)
Experimental Results: A single oral dose of 15 mg/kg on day 7 reduced established mechanical hyperalgesia 4 hours after administration. Repeated administration of 15 mg/kg once daily from day 15-18 maintained a significant antihyperalgesia effect for 5 days, comparable to duloxetine.

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Animal/Disease Models:Sprague Dawley (male, weight 200-220 g at surgery; weight 233-289 g at administration, chronic compression injury of the left sciatic nerve) [1]
Doses: 20 mg/kg (repeated administration; reversal of hyperalgesia); 20 mg/kg (single administration; lipid analysis)
Route of Administration: Oral; once daily for 5 days (days 14-18); single administration 14 days after CCI
Experimental Results: Repeated administration of 20 mg/kg reversed hyperalgesia and restored the von Frey threshold to the sham surgery level, with efficacy comparable to naproxen and pregabalin. A single administration of 20 mg/kg reduced the concentration of 2-AG in the damaged sciatic nerve and restored the concentration of AA to normal; CCI resulted in a 7-fold increase in the concentration of 2-AG and a 2-fold increase in the concentration of AA.

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Animal/Disease Models:Sprague Dawley mice (male, 250-315 g, chronic compression injury of the left sciatic nerve, right jugular vein catheter implanted) [1]
Doses: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
Route of Administration: Intravenous injection; single bolus injection after baseline vector recording
Experimental Results: Dose-dependent high-threshold (HT) and wide dynamic range-like (WDR-like) single-cell response modulation was produced, with significant inhibition at 1 mg/kg. Low-threshold mechanoreceptor (LTMR) single-cell activity was not modulated at 1 mg/kg.

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Animal/Disease Models:Sprague Dawley (male, 208-263 g, subcutaneous injection of pentylenetetrazol 80 mg/kg) [1]
Doses: 8 mg/kg; 16 mg/kg; 30 mg/kg
Route of Administration: Oral; single dose, 4 hours before pentylenetetrazol injection
Experimental Results: No changes were made to seizure latency or incidence at any of the tested doses. No changes were made to 2-AG levels in the brain after administration.

[1]. Suppression of pain transmission and behavior by inhibition of peripheral diacylglycerol metabolism. Cell Chem Biol. 2026;33(1):74-90.e19.

Typically exists as solids at room temperature

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)