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MedKoo Cat#: 530638 | Name: AS-2444697 HCl
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Description:

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

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

AS-2444697 HCl
AS-2444697 HCl
CAS#1287665-60-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 530638

Name: AS-2444697 HCl

CAS#: 1287665-60-4 (HCl)

Chemical Formula: C19H21ClN6O4

Exact Mass: 0.0000

Molecular Weight: 432.87

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 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 1,050.00 2 Weeks
100mg USD 1,850.00 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/
Solvent mg/mL mM
Solubility
DMSO 16.8 38.88
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 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.
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.

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