AS-2444697 HCl
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MedKoo CAT#: 530638

CAS#: 1287665-60-4 (HCl)

Description: AS-2444697 is a RAK-4 inhibitor. Six weeks' repeated administration of AS2444697 (0.3-3 mg/kg, twice daily) dose-dependently and significantly reduced urinary protein excretion and prevented the development of glomerulosclerosis and interstitial fibrosis without affecting the blood pressure. AS2444697 significantly reduced or showed a decreasing trend in expression and levels of these inflammatory parameters. AS2444697 suppresses the progression of chronic renal failure via anti-inflammatory action and may therefore be potentially useful in treating CKD patients.

Chemical Structure

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AS-2444697 HCl
CAS# 1287665-60-4 (HCl)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 530638
Name: AS-2444697 HCl
CAS#: 1287665-60-4 (HCl)
Chemical Formula: C19H21ClN6O4
Exact Mass: 0.00
Molecular Weight: 432.865
Elemental Analysis: C, 52.72; H, 4.89; Cl, 8.19; N, 19.42; O, 14.78

Price and Availability

Size Price Availability Quantity
10mg USD 450 2 Weeks
25mg USD 750 2 Weeks
50mg USD 1250 2 Weeks
100mg USD 2150 2 Weeks
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Related CAS #: 1287665-60-4 (HCl)   1287665-58-0 (free base)    

Synonym: AS-2444697; AS 2444697; AS2444697; AS-2444697 HCl; AS-2444697 hydrochloride.

IUPAC/Chemical Name: N-(3-carbamoyl-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)-2-(2-methylpyridin-4-yl)oxazole-4-carboxamide hydrochloride

InChi Key: FGNHLIIFEDYNFZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H20N6O4.ClH/c1-11-8-12(2-5-21-11)19-23-15(10-29-19)18(27)22-14-9-25(24-16(14)17(20)26)13-3-6-28-7-4-13;/h2,5,8-10,13H,3-4,6-7H2,1H3,(H2,20,26)(H,22,27);1H

SMILES Code: O=C(C1=COC(C2=CC(C)=NC=C2)=N1)NC3=CN(C4CCOCC4)N=C3C(N)=O.[H]Cl

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: 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: Renal inflammation is a final common pathway of chronic kidney disease (CKD), and its progression can be used to effectively gauge the degree of renal dysfunction. Interleukin-1 (IL-1) receptor-associated kinase 4 (IRAK-4) has been reported to be a pivotal molecule for IL-1 receptor- and Toll-like receptor-induced signaling and activation of proinflammatory mediators.

Product Data:
Product Data
Certificate of Analysis:
View CoA: current batch, Lot#A22O3B14
Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)
Instruction:
View handling instruction
Biological target: AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM.
In vitro activity: TBD
In vivo activity: Chronic administration of AS2444697 dose-dependently and significantly attenuated urinary albumin excretion and hyperfiltration, alleviated renal hypertrophy, and decreased markers of renal tubular and glomerular podocyte injury. Diabetic mice exhibited renal tissue lesions, glomerulosclerosis, tubular dilatation, cell infiltration, and basophilic change (Fig. 4). Chronic administration of AS2444697 dose-dependently and significantly improved these indicators of renal injury. Further, diabetic mice showed signs of inflammation, as demonstrated by elevated plasma levels of proinflammatory cytokines (IL-1β, IL-6, IL-18, TNF-α, and MCP-1) and inflammatory marker CRP (Fig. 5). AS2444697 dose-dependently and significantly decreased these elevated plasma proinflammatory cytokine and inflammatory marker levels. Diabetic mice also exhibited increased plasma levels of endothelial dysfunction parameters (ICAM-1, VCAM-1, E-selectin, and P-selectin) (Fig. 6) and plasma and renal levels of oxidative stress biomarkers (TBARS and protein carbonyl) (Fig. 7). AS2444697 dose-dependently and significantly reduced these endothelial dysfunction parameters and oxidative stress biomarkers. Reference: Naunyn Schmiedebergs Arch Pharmacol. 2020 Jul;393(7):1197-1209. https://pubmed.ncbi.nlm.nih.gov/31974740/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 16.8 38.88

Preparing Stock Solutions

The following data is based on the product molecular weight 432.87 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. Kondo M, Tahara A, Hayashi K, Inami H, Ishikawa T, Tomura Y. Therapeutic effects of interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 on diabetic nephropathy in type 2 diabetic mice. Naunyn Schmiedebergs Arch Pharmacol. 2020 Jul;393(7):1197-1209. doi: 10.1007/s00210-020-01816-2. Epub 2020 Jan 23. PMID: 31974740. 2. Kondo M, Tahara A, Hayashi K, Abe M, Inami H, Ishikawa T, Ito H, Tomura Y. Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch Pharmacol. 2014 Oct;387(10):909-19. doi: 10.1007/s00210-014-1023-z. Epub 2014 Jul 23. PMID: 25052043.
In vitro protocol: TBD
In vivo protocol: 1. Kondo M, Tahara A, Hayashi K, Inami H, Ishikawa T, Tomura Y. Therapeutic effects of interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 on diabetic nephropathy in type 2 diabetic mice. Naunyn Schmiedebergs Arch Pharmacol. 2020 Jul;393(7):1197-1209. doi: 10.1007/s00210-020-01816-2. Epub 2020 Jan 23. PMID: 31974740. 2. Kondo M, Tahara A, Hayashi K, Abe M, Inami H, Ishikawa T, Ito H, Tomura Y. Renoprotective effects of novel interleukin-1 receptor-associated kinase 4 inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats. Naunyn Schmiedebergs Arch Pharmacol. 2014 Oct;387(10):909-19. doi: 10.1007/s00210-014-1023-z. Epub 2014 Jul 23. PMID: 25052043.

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1: Kondo M, Tahara A, Hayashi K, Abe M, Inami H, Ishikawa T, Ito H, Tomura Y.
Renoprotective effects of novel interleukin-1 receptor-associated kinase 4
inhibitor AS2444697 through anti-inflammatory action in 5/6 nephrectomized rats.
Naunyn Schmiedebergs Arch Pharmacol. 2014 Oct;387(10):909-19. doi:
10.1007/s00210-014-1023-z. Epub 2014 Jul 23. PubMed PMID: 25052043.