| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Palmitoyl thio‑PC targets the active site of secreted PLA2 (sPLA2) enzymes, particularly bee venom sPLA2 and mammalian group IIA PLA2. The thioester bond at the sn‑2 position is hydrolyzed by PLA2, releasing a free thiol group that is detected via DTNB, producing a colorimetric signal proportional to enzyme activity.
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|---|---|
| ln Vitro |
In vitro, Palmitoyl thio‑PC is used to measure PLA2 activity. In a mixed micelle system (phospholipid:Triton X‑100), 0.1-1 mM substrate is incubated with 0.1-10 microg/mL sPLA2 in 100 mM Tris‑HCl (pH 7.5) containing 10 mM CaCl2 and 10 mM DTNB. Absorbance at 412 nm is monitored continuously for 5-10 min. The enzyme activity is calculated from the slope of the linear region.
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| ln Vivo |
Palmitoyl thio‑PC is not used for therapeutic in vivo animal studies; it is a biochemical reagent for enzyme activity assays. It can be used in ex vivo tissue homogenates or bronchoalveolar lavage fluid to measure sPLA2 activity in inflammation or sepsis models, but it is not directly administered to animals for pharmacological testing.
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| Enzyme Assay |
A cell‑free PLA2 activity assay protocol: 1 mM Palmitoyl thio‑PC is mixed with 0.5 mM Triton X‑100 and 10 mM DTNB in 100 mM Tris‑HCl (pH 7.5), 10 mM CaCl2. The reaction is initiated by adding 10 ng bee venom sPLA2. Absorbance at 412 nm is read every 30 sec for 10 min at 25 degC. Specific activity (nmol/min/mg) is calculated using ε412 = 13,600 M-¹cm-¹ for the product 2‑nitro‑5‑thiobenzoate.
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| Cell Assay |
No direct cellular assay is performed with Palmitoyl thio‑PC. For cell‑based sPLA2 activity studies, cells (e.g., macrophages) are stimulated with LPS (100 ng/mL) for 6-24 h to induce sPLA2 expression. Culture medium is collected, and an aliquot (10-50 microL) is incubated with Palmitoyl thio‑PC/DTNB reaction buffer for 15-30 min at 37 degC. The increase in A412 correlates with secreted sPLA2 activity.
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| Animal Protocol |
Palmitoyl thio‑PC is not used in live animals. In an ex vivo study, rats are subjected to a carrageenan‑induced air pouch model of inflammation. Pouch exudate (100 microL) is collected 6 h after carrageenan injection and incubated with 1 mM Palmitoyl thio‑PC and 10 mM DTNB. Absorbance at 412 nm is measured to quantify sPLA2 activity in the inflammatory exudate, reflecting PLA2‑mediated eicosanoid biosynthesis.
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| ADME/Pharmacokinetics |
Palmitoyl thio‑PC is a synthetic lipid, not a drug; its pharmacokinetics are irrelevant. The molecular formula is C40H₈0NO₇PS, MW 750.10. It is typically stored as a solid at −20 degC. It should be protected from light and moisture. Its melting point is around 100‑105 degC. The compound is stable in organic solvents such as chloroform or DMSO.
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| Toxicity/Toxicokinetics |
Palmitoyl thio‑PC has not been evaluated for acute toxicity. As a laboratory reagent, it is generally considered low‑toxicity when handled properly. It may cause skin and eye irritation (H315, H319). Avoid inhalation and contact. Wear gloves, goggles, and lab coat. Dispose of waste according to local regulations. No LD₅0 value is available in the literature.
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| References | |
| Additional Infomation |
Chromogenic substrate for phospholipase A2
Palmitoyl thio‑PC is not a drug; it is a research‑only chromogenic substrate for measuring PLA2 activity. It is a convenient, non‑radioactive alternative to radiolabeled phosphatidylcholine substrates. It is used in drug discovery to screen for PLA2 inhibitors, in inflammation research to assess sPLA2 activity in disease models, and in enzyme kinetic studies. The product is sold for laboratory use only and not for human diagnostics or therapy. |
| Molecular Formula |
C40H80NO7PS
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|---|---|
| Molecular Weight |
750.10
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| Exact Mass |
749.539
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| CAS # |
113881-60-0
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| PubChem CID |
195048
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
12.398
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
40
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| Heavy Atom Count |
50
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| Complexity |
831
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)([O-])OCC[N+](C)(C)C)SC(=O)CCCCCCCCCCCCCCC
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| InChi Key |
CJNCGLSWHABGOT-KXQOOQHDSA-N
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| InChi Code |
InChI=1S/C40H80NO7PS/c1-6-8-10-12-14-16-18-20-22-24-26-28-30-32-39(42)46-36-38(37-48-49(44,45)47-35-34-41(3,4)5)50-40(43)33-31-29-27-25-23-21-19-17-15-13-11-9-7-2/h38H,6-37H2,1-5H3/t38-/m1/s1
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| Chemical Name |
[(2R)-3-hexadecanoyloxy-2-hexadecanoylsulfanylpropyl] 2-(trimethylazaniumyl)ethyl phosphate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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
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|---|---|
| Solubility (In Vivo) |
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.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] Oral Formulations
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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3332 mL | 6.6658 mL | 13.3316 mL | |
| 5 mM | 0.2666 mL | 1.3332 mL | 2.6663 mL | |
| 10 mM | 0.1333 mL | 0.6666 mL | 1.3332 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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