| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg |
| Targets |
(E/Z)-HA155 targets autotaxin (ATX), also known as ENPP2, a lysophospholipase D that catalyzes the conversion of lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA). LPA is a bioactive lipid that signals through LPA receptors to regulate cell proliferation, migration, survival, and inflammation. By inhibiting ATX, the compound reduces LPA production and has potential applications in cancer, fibrosis, inflammation, pain, and angiogenesis research.
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| ln Vitro |
In vitro, (E/Z)-HA155 is a potent inhibitor of autotaxin (ATX) type I. It inhibits ATX enzymatic activity, reducing the production of LPA from LPC. However, specific IC50 values and detailed in vitro activity data are not extensively reported in the available literature. The compound shows potential for research on cancer, fibrosis, inflammation, pain, and angiogenesis.
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| ln Vivo |
In vivo, (E/Z)-HA155 is expected to show efficacy in animal models of cancer, fibrosis, inflammation, and pain by reducing LPA production. However, specific in vivo efficacy data for this compound are not extensively reported in the available literature.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for (E/Z)-HA155 typically involve ATX activity assays using purified recombinant ATX enzyme. The assay is performed in 96-well plates with assay buffer (50 mM Tris-HCl pH 8.0, 140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2). The compound (typically 0.001-100 μM) is incubated with the enzyme and the substrate (e.g., FS-3, a fluorogenic LPC analog) at 37°C for 30-60 minutes. Fluorescence is measured at excitation 485 nm and emission 535 nm. The IC50 is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for (E/Z)-HA155 use cancer cell lines or fibroblasts to assess effects on LPA-mediated signaling. Cells are cultured in appropriate media and treated with various concentrations of the compound (typically 0.01-10 μM) for 4-24 hours. LPA production in culture supernatant is measured by LC-MS. Cell proliferation, migration, and invasion are assessed using standard assays. LPA receptor signaling (e.g., ERK phosphorylation) is measured by Western blotting.
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| Animal Protocol |
In vivo animal studies with (E/Z)-HA155 would typically use mouse models of cancer, fibrosis, or inflammation. The compound would be administered orally or intraperitoneally at doses of 1-30 mg/kg daily for 2-4 weeks. Tumor growth, fibrotic tissue, or inflammatory markers would be assessed. LPA levels in plasma or tissues would be measured. However, specific in vivo data for this compound are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of (E/Z)-HA155: The compound has a molecular weight of 463.29. Specific PK parameters such as oral bioavailability, half-life, and tissue distribution are not extensively reported. As a small molecule, it is expected to have moderate bioavailability.
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| Toxicity/Toxicokinetics |
The toxicity profile of (E/Z)-HA155 is not extensively reported. The compound is for research use only and not for human therapeutic use. Standard toxicity studies would include acute toxicity in rodents and cytotoxicity assays.
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| References | |
| Additional Infomation |
(E/Z)-HA155 (CAS 1229652-22-5) is a potent type I inhibitor of autotaxin (ATX) with potential applications in cancer, fibrosis, inflammation, pain, and angiogenesis research. It has a molecular formula of C24H19BFNO5S and a molecular weight of 463.29. The compound is available for research purposes only.
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| Molecular Formula |
C24H19BFNO5S
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|---|---|
| Molecular Weight |
463.28576874733
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| Exact Mass |
463.106
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| CAS # |
1229652-22-5
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| Related CAS # |
HA155;1312201-00-5
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| PubChem CID |
46856189
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
691.0±65.0 °C at 760 mmHg
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| Flash Point |
371.7±34.3 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.683
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| LogP |
5.25
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
714
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| Defined Atom Stereocenter Count |
0
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| SMILES |
B(C1=CC=C(C=C1)COC2=CC=C(C=C2)/C=C\3/C(=O)N(C(=O)S3)CC4=CC=C(C=C4)F)(O)O
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| InChi Key |
BRWUZCBSWABPMR-XKZIYDEJSA-N
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| InChi Code |
InChI=1S/C24H19BFNO5S/c26-20-9-3-17(4-10-20)14-27-23(28)22(33-24(27)29)13-16-5-11-21(12-6-16)32-15-18-1-7-19(8-2-18)25(30)31/h1-13,30-31H,14-15H2/b22-13-
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| Chemical Name |
[4-[[4-[(Z)-[3-[(4-fluorophenyl)methyl]-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy]methyl]phenyl]boronic acid
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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 | 2.1585 mL | 10.7924 mL | 21.5848 mL | |
| 5 mM | 0.4317 mL | 2.1585 mL | 4.3170 mL | |
| 10 mM | 0.2158 mL | 1.0792 mL | 2.1585 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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