HA130 | CAS#1229652-21-4 | autotaxin inhibitor

MedKoo Cat#: 522395 | Name: HA130

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

HA130

CAS#1229652-21-4

Theoretical Analysis

MedKoo Cat#: 522395

Name: HA130

CAS#: 1229652-21-4

Chemical Formula: C24H19BFNO5S

Exact Mass: 463.1061

Molecular Weight: 463.29

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
50mg	USD 350.00	2 Weeks
100mg	USD 550.00	2 Weeks
200mg	USD 950.00	2 Weeks
500mg	USD 1,650.00	2 Weeks
1g	USD 2,450.00	2 Weeks
2g	USD 3,950.00	2 Weeks

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Related CAS #

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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

Product Data

Instruction

View handling instruction

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/

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

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

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.