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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
HA155 targets autotaxin (ATX), an enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA). It acts as a potent and selective inhibitor with an IC50 of 5.7 nM. By inhibiting ATX, HA155 blocks the production of LPA, a bioactive lipid mediator involved in inflammation, fibrosis, cancer progression, and thrombosis.
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| ln Vitro |
By attaching to the ATX active site, HA-155 suppresses ATX[1]. In a dose-dependent manner, HA155 totally inhibited the thrombin-mediated increase in platelet-derived LPA [3].
In vitro, HA155 inhibits autotaxin with an IC50 of 5.7 nM. It binds directly to the ATX active site, blocking the enzymatic generation of LPA. These in vitro activities confirm its profile as a potent and selective ATX inhibitor. Its effects on LPA production and downstream signaling have been demonstrated in various assays. |
| ln Vivo |
In vivo, HA155 has anticancer, anti-inflammatory, and anti-fibrotic effects. By inhibiting ATX and reducing LPA production, HA155 modulates inflammation, fibrosis, and cancer progression. However, specific details of in vivo efficacy studies, such as the animal models used and the dosing regimens, are not extensively detailed in the available literature.
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| Enzyme Assay |
The in vitro enzyme assay for HA155 measures its ability to inhibit autotaxin activity. These cell-free assays use purified ATX and a substrate such as lysophosphatidylcholine. The compound's inhibitory potency (IC50) is determined by measuring the reduction in enzyme activity. HA155 shows an IC50 of 5.7 nM for ATX inhibition.
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| Cell Assay |
In vitro cellular assays for HA155 assess its effects on ATX-mediated signaling. Cells are treated with HA155, and the production of LPA or downstream signaling is measured. These assays demonstrate the compound's ability to inhibit ATX activity and reduce LPA-mediated signaling in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for HA155 have been conducted in models of inflammation, fibrosis, and cancer to assess its efficacy. However, specific details of these studies are not extensively detailed in the available literature. The compound is a research tool for studying the role of ATX and LPA in various diseases.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for HA155 are not extensively detailed in the available literature. As a boronic acid-based compound, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as oral bioavailability, half-life, and distribution are not provided. The compound is primarily used in research settings.
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| Toxicity/Toxicokinetics |
Specific toxicity data for HA155 are not extensively detailed in the available literature. As a selective ATX inhibitor, its toxicity profile is likely related to its mechanism of action. However, preclinical toxicology studies would be required to assess its safety margin. The compound is intended for research use only.
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| References | |
| Additional Infomation |
HA155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM. It is a boronic acid-based compound that effectively blocks the enzymatic generation of lysophosphatidic acid (LPA). It has anticancer, anti-inflammatory, and anti-fibrotic effects. It is a research compound for studying ATX and LPA signaling and is not approved for clinical use.
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| Molecular Formula |
C24H18NO3FS.H3BO2
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|---|---|
| Molecular Weight |
465.30164
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| Exact Mass |
463.106
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| CAS # |
1312201-00-5
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| Related CAS # |
(E/Z)-HA155;1229652-22-5
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| PubChem CID |
46856189
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| Appearance |
White to off-white solid powder
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| LogP |
3.258
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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 | 2.1492 mL | 10.7458 mL | 21.4915 mL | |
| 5 mM | 0.4298 mL | 2.1492 mL | 4.2983 mL | |
| 10 mM | 0.2149 mL | 1.0746 mL | 2.1492 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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