HA130
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MedKoo CAT#: 522395

CAS#: 1229652-21-4

Description: HA130 is a potent and selective autotaxin (ATX) inhibitor (IC50 = 28 nM). HA130 slows T cell migration across lymph node HEVs in vivo. Ex vivo, HA130 blunts the TEM-promoting activity of ATX, paralleling its in vivo effects.


Chemical Structure

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HA130
CAS# 1229652-21-4

Theoretical Analysis

MedKoo Cat#: 522395
Name: HA130
CAS#: 1229652-21-4
Chemical Formula: C24H19BFNO5S
Exact Mass: 463.11
Molecular Weight: 463.286
Elemental Analysis: C, 62.22; H, 4.13; B, 2.33; F, 4.10; N, 3.02; O, 17.27; S, 6.92

Price and Availability

Size Price Availability Quantity
50mg USD 350
100mg USD 550
200mg USD 950
500mg USD 1650
1g USD 2450
2g USD 3950
5g USD 6450
Bulk inquiry

Synonym: HA130; HA-130; HA 130.

IUPAC/Chemical Name: (Z)-(3-((4-((3-(4-fluorobenzyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenoxy)methyl)phenyl)boronic acid

InChi Key: VTNKMYWFWQTEHE-XKZIYDEJSA-N

InChi Code: InChI=1S/C24H19BFNO5S/c26-20-8-4-17(5-9-20)14-27-23(28)22(33-24(27)29)13-16-6-10-21(11-7-16)32-15-18-2-1-3-19(12-18)25(30)31/h1-13,30-31H,14-15H2/b22-13-

SMILES Code: OB(C1=CC=CC(COC2=CC=C(/C=C(SC(N3CC4=CC=C(F)C=C4)=O)/C3=O)C=C2)=C1)O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: HA130 is a selective autotaxin (ATX) inhibitor with an IC50 of 28 nM.
In vitro activity: HA130 inhibited IL-8 secretion by 45% and 76% in cells stimulated with lysoPS and PLA1A, respectively (Figure 5C,D). Reference: Int J Mol Sci. 2021 Nov 24;22(23):12685. https://pubmed.ncbi.nlm.nih.gov/34884486/
In vivo activity: Treatment with HA130 or PF8380 significantly reverted the basal respiration, spare respiratory capacity, ATP turnover, and maximal respiration to near‐normal levels compared with results in the I/R group (Figure 3D through 3F). Reference: J Am Heart Assoc. 2021 Sep 21;10(18):e021511. https://pubmed.ncbi.nlm.nih.gov/34514847/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 10.0 21.58
DMSO 30.1 64.99
Ethanol 0.5 1.08

Preparing Stock Solutions

The following data is based on the product molecular weight 463.29 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Zhao Y, Hasse S, Vaillancourt M, Zhao C, Davis L, Boilard E, Fortin P, Di Battista J, Poubelle PE, Bourgoin SG. Phospholipase A1 Member A Activates Fibroblast-like Synoviocytes through the Autotaxin-Lysophosphatidic Acid Receptor Axis. Int J Mol Sci. 2021 Nov 24;22(23):12685. doi: 10.3390/ijms222312685. PMID: 34884486; PMCID: PMC8657932. 2. Vázquez-Medina JP, Dodia C, Weng L, Mesaros C, Blair IA, Feinstein SI, Chatterjee S, Fisher AB. The phospholipase A2 activity of peroxiredoxin 6 modulates NADPH oxidase 2 activation via lysophosphatidic acid receptor signaling in the pulmonary endothelium and alveolar macrophages. FASEB J. 2016 Aug;30(8):2885-98. doi: 10.1096/fj.201500146R. Epub 2016 May 13. PMID: 27178323; PMCID: PMC4970605. 3. Bhattarai S, Sharma S, Ara H, Subedi U, Sun G, Li C, Bhuiyan MS, Kevil C, Armstrong WP, Minvielle MT, Miriyala S, Panchatcharam M. Disrupted Blood-Brain Barrier and Mitochondrial Impairment by Autotaxin-Lysophosphatidic Acid Axis in Postischemic Stroke. J Am Heart Assoc. 2021 Sep 21;10(18):e021511. doi: 10.1161/JAHA.121.021511. Epub 2021 Sep 13. PMID: 34514847; PMCID: PMC8649548. 4. Zhang Y, Chen YC, Krummel MF, Rosen SD. Autotaxin through lysophosphatidic acid stimulates polarization, motility, and transendothelial migration of naive T cells. J Immunol. 2012 Oct 15;189(8):3914-24. doi: 10.4049/jimmunol.1201604. Epub 2012 Sep 7. PMID: 22962684; PMCID: PMC3509168.
In vitro protocol: 1. Zhao Y, Hasse S, Vaillancourt M, Zhao C, Davis L, Boilard E, Fortin P, Di Battista J, Poubelle PE, Bourgoin SG. Phospholipase A1 Member A Activates Fibroblast-like Synoviocytes through the Autotaxin-Lysophosphatidic Acid Receptor Axis. Int J Mol Sci. 2021 Nov 24;22(23):12685. doi: 10.3390/ijms222312685. PMID: 34884486; PMCID: PMC8657932. 2. Vázquez-Medina JP, Dodia C, Weng L, Mesaros C, Blair IA, Feinstein SI, Chatterjee S, Fisher AB. The phospholipase A2 activity of peroxiredoxin 6 modulates NADPH oxidase 2 activation via lysophosphatidic acid receptor signaling in the pulmonary endothelium and alveolar macrophages. FASEB J. 2016 Aug;30(8):2885-98. doi: 10.1096/fj.201500146R. Epub 2016 May 13. PMID: 27178323; PMCID: PMC4970605.
In vivo protocol: 1. Bhattarai S, Sharma S, Ara H, Subedi U, Sun G, Li C, Bhuiyan MS, Kevil C, Armstrong WP, Minvielle MT, Miriyala S, Panchatcharam M. Disrupted Blood-Brain Barrier and Mitochondrial Impairment by Autotaxin-Lysophosphatidic Acid Axis in Postischemic Stroke. J Am Heart Assoc. 2021 Sep 21;10(18):e021511. doi: 10.1161/JAHA.121.021511. Epub 2021 Sep 13. PMID: 34514847; PMCID: PMC8649548. 2. Zhang Y, Chen YC, Krummel MF, Rosen SD. Autotaxin through lysophosphatidic acid stimulates polarization, motility, and transendothelial migration of naive T cells. J Immunol. 2012 Oct 15;189(8):3914-24. doi: 10.4049/jimmunol.1201604. Epub 2012 Sep 7. PMID: 22962684; PMCID: PMC3509168.

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1: Park SJ, Lee KP, Kang S, Chung HY, Bae YS, Okajima F, Im DS.
Lysophosphatidylethanolamine utilizes LPA(1) and CD97 in MDA-MB-231 breast cancer
cells. Cell Signal. 2013 Nov;25(11):2147-54. doi: 10.1016/j.cellsig.2013.07.001.
Epub 2013 Jul 6. PubMed PMID: 23838008.


2: Lai SL, Yao WL, Tsao KC, Houben AJ, Albers HM, Ovaa H, Moolenaar WH, Lee SJ.
Autotaxin/Lpar3 signaling regulates Kupffer's vesicle formation and left-right
asymmetry in zebrafish. Development. 2012 Dec 1;139(23):4439-48. doi:
10.1242/dev.081745. Epub 2012 Oct 24. PubMed PMID: 23095890.


3: Zhang Y, Chen YC, Krummel MF, Rosen SD. Autotaxin through lysophosphatidic
acid stimulates polarization, motility, and transendothelial migration of naive T
cells. J Immunol. 2012 Oct 15;189(8):3914-24. doi: 10.4049/jimmunol.1201604. Epub
2012 Sep 7. PubMed PMID: 22962684; PubMed Central PMCID: PMC3509168.