IXA4
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MedKoo CAT#: 556064

CAS#: 1185329-96-7

Description: IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 transiently activates protective IRE1/XBP1s signaling in liver without inducing RIDD or TRAF2/JNK signaling. IXA4 treatment improves systemic glucose metabolism and liver insulin action through IRE1-dependent remodeling of the hepatic transcriptome that reduces glucose production and steatosis. IXA4-stimulated IRE1 activation also enhances pancreatic function. Our findings indicate that systemic, transient activation of IRE1/XBP1s signaling engenders multi-tissue benefits that integrate to mitigate obesity-driven metabolic dysfunction.


Chemical Structure

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IXA4
CAS# 1185329-96-7

Theoretical Analysis

MedKoo Cat#: 556064
Name: IXA4
CAS#: 1185329-96-7
Chemical Formula: C24H28N4O4
Exact Mass: 436.2111
Molecular Weight: 436.512
Elemental Analysis: C, 66.04; H, 6.47; N, 12.84; O, 14.66

Price and Availability

Size Price Availability Quantity
5.0mg USD 120.0 Ready to ship
10.0mg USD 190.0 Ready to ship
25.0mg USD 350.0 Ready to ship
50.0mg USD 550.0 Ready to ship
100.0mg USD 950.0 Ready to ship
200.0mg USD 1450.0 Ready to ship
500.0mg USD 2850.0 Ready to ship
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Synonym: IXA4; IXA-4; IXA 4;

IUPAC/Chemical Name: N-(1-(2-(methyl(2-(p-tolyloxy)ethyl)amino)-2-oxoethyl)-1H-pyrazol-4-yl)-3-phenoxypropanamide

InChi Key: ZVSKMVAWWBSNOY-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H28N4O4/c1-19-8-10-22(11-9-19)32-15-13-27(2)24(30)18-28-17-20(16-25-28)26-23(29)12-14-31-21-6-4-3-5-7-21/h3-11,16-17H,12-15,18H2,1-2H3,(H,26,29)

SMILES Code: CC1=CC=C(OCCN(C(CN2N=CC(NC(=O)CCOC3=CC=CC=C3)=C2)=O)C)C=C1

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

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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

Biological target: IXA4 is a highly selective, non-toxic IRE1/XBP1s activator. IXA4 (10 μM; 4 hours) selectively upregulates XBP1s mRNA, relative to genes regulated by ATF6 (e.g., BiP) or PERK (e.g., CHOP), in other cell lines including Huh7 and SHSY5Y cells.
In vitro activity: IXA4 reduced Aβ levels 50% in conditioned media prepared on CHO7PA2 cells expressing the V717F APP (APPV717F) mutant (Fig. 5B). This study confirmed compound-dependent IRE1/XBP1s activation in these cells by qPCR (Extended Data Fig. 7C). Reference: Nat Chem Biol. 2020 Oct;16(10):1052-1061. https://pubmed.ncbi.nlm.nih.gov/32690944/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
dmso 93.5 214.2
Ethanol 11.0 25.2

Preparing Stock Solutions

The following data is based on the product molecular weight 436.512 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. Grandjean JMD, Madhavan A, Cech L, Seguinot BO, Paxman RJ, Smith E, Scampavia L, Powers ET, Cooley CB, Plate L, Spicer TP, Kelly JW, Wiseman RL. Pharmacologic IRE1/XBP1s activation confers targeted ER proteostasis reprogramming. Nat Chem Biol. 2020 Oct;16(10):1052-1061. doi: 10.1038/s41589-020-0584-z. Epub 2020 Jul 20. PMID: 32690944; PMCID: PMC7502540.
In vitro protocol: 1. Grandjean JMD, Madhavan A, Cech L, Seguinot BO, Paxman RJ, Smith E, Scampavia L, Powers ET, Cooley CB, Plate L, Spicer TP, Kelly JW, Wiseman RL. Pharmacologic IRE1/XBP1s activation confers targeted ER proteostasis reprogramming. Nat Chem Biol. 2020 Oct;16(10):1052-1061. doi: 10.1038/s41589-020-0584-z. Epub 2020 Jul 20. PMID: 32690944; PMCID: PMC7502540.
In vivo protocol: TBD

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1: Madhavan A, Kok BP, Rius B, Grandjean JMD, Alabi A, Albert V, Sukiasyan A, Powers ET, Galmozzi A, Saez E, Wiseman RL. Pharmacologic IRE1/XBP1s activation promotes systemic adaptive remodeling in obesity. Nat Commun. 2022 Feb 1;13(1):608. doi: 10.1038/s41467-022-28271-2. PMID: 35105890; PMCID: PMC8807832.

2: Grandjean JMD, Wiseman RL. Small molecule strategies to harness the unfolded protein response: where do we go from here? J Biol Chem. 2020 Nov 13;295(46):15692-15711. doi: 10.1074/jbc.REV120.010218. Epub 2020 Sep 4. PMID: 32887796; PMCID: PMC7667976.

IXA4

5.0mg / USD 120.0