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Chemical Structure| 1229652-21-4 Chemical Structure| 1229652-21-4

Structure of HA130
CAS No.: 1229652-21-4

Chemical Structure| 1229652-21-4

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HA130 is a selective autotaxin (ATX) inhibitor with an IC50 of 28 nM.

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Product Details of HA130

CAS No. :1229652-21-4
Formula : C24H19BFNO5S
M.W : 463.29
SMILES Code : OB(O)C1=CC=CC(COC2=CC=C(C=C2)/C=C(C3=O)\SC(N3CC4=CC=C(C=C4)F)=O)=C1
MDL No. :MFCD20926343
InChI Key :VTNKMYWFWQTEHE-XKZIYDEJSA-N
Pubchem ID :46911532

Safety of HA130

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary mouse CD3+ T cells 10 μM 7 minutes ATX/LPC induced polarization of primary mouse CD3+ T cells, with higher polarization rates when combined with CCL21. PMC3509168
TK1 lymphoma cells 0.1 μM to 10 μM 7 minutes ATX/LPC induced polarization of TK1 cells, doubling the polarization rate to 34% within 30 seconds and reaching 75% after 10 minutes. PMC3509168
Human primary fibroblast-like synoviocytes (FLSs) 0.2 µg/mL or 0.5 µg/mL 24 hours To evaluate the effect of PLA1A on IL-8 secretion by FLSs, results showed PLA1A induced IL-8 secretion in a concentration-dependent manner. PMC8657932

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Ischemic stroke model Intraperitoneal injection 0.5 mg/kg body weight Single dose, observed for 24 hours HA130 significantly reduced autotaxin activity in the ischemia and reperfusion (I/R) group, decreased plasma LPA levels, and improved mitochondrial function. PMC8649548
C57BL/6 mice Thioacetamide-induced acute hepatic encephalopathy model Intraperitoneal injection 463 µg/kg Twice daily for 3 days HA130 improved the main hallmarks of hepatic encephalopathy, including alleviating inflammation, gut leukocyte infiltration, liver inflammation, neuroinflammation, hyperammonemia, and cerebral ammonia levels PMC10394058

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.79mL

2.16mL

1.08mL

21.58mL

4.32mL

2.16mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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