MedKoo Cat#: 555871 | Name: Isuzinaxib
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Description:

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

APX-115, also known as EWHA-18278, is a potent, orally active pan NADPH oxidase (Nox) inhibitor. APX-115 protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice. APX-115 might be a promising therapeutic agent for the treatment of DN because of its pan-NOX inhibitory activity, including its NOX5 inhibitory activity, and also owing to its anti-inflammatory effect.

Chemical Structure

Isuzinaxib
Isuzinaxib
CAS#1270084-92-8 (free base)

Theoretical Analysis

MedKoo Cat#: 555871

Name: Isuzinaxib

CAS#: 1270084-92-8 (free base)

Chemical Formula: C17H17N3O

Exact Mass: 279.1372

Molecular Weight: 279.34

Elemental Analysis: C, 73.10; H, 6.13; N, 15.04; O, 5.73

Price and Availability

Size Price Availability Quantity
50g USD 550.00 2 Weeks
100mg USD 950.00 2 Weeks
200mg USD 1,850.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 3,650.00 2 Weeks
2g USD 5,950.00 2 Weeks
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Synonym
APX-115 free base; APX 115; APX115; EWHA-18278; EWHA 18278; EWHA18278; Isuzinaxib
IUPAC/Chemical Name
3-phenyl-4-propyl-1-(pyridin-2-yl)-1H-pyrazol-5-ol
InChi Key
LQKQLKMTJOMCMJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H17N3O/c1-2-8-14-16(13-9-4-3-5-10-13)19-20(17(14)21)15-11-6-7-12-18-15/h3-7,9-12,21H,2,8H2,1H3
SMILES Code
OC1=C(CCC)C(C2=CC=CC=C2)=NN1C3=NC=CC=C3
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
>3 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
NADPH oxidases (NOXs) are comprised of different isoforms, NOX1 to 5 and Duox1 and 2, and they trigger diabetic nephropathy (DN) in the patients with diabetes mellitus. Recently, it was shown that, compared to the other isoforms, the expression of NOX5 was increased in the patients with DN and, NOX5 has been suggested to be important in the development of therapeutic agents.

Preparing Stock Solutions

The following data is based on the product molecular weight 279.34 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
1: Lee ES, Kim HM, Lee SH, Ha KB, Bae YS, Lee SJ, Moon SH, Lee EY, Lee JH, Chung CH. APX-115, a pan-NADPH oxidase inhibitor, protects development of diabetic nephropathy in podocyte specific NOX5 transgenic mice. Free Radic Biol Med. 2020 Oct 2;161:92-101. doi: 10.1016/j.freeradbiomed.2020.09.024. Epub ahead of print. PMID: 33011273. 2: Chocry M, Leloup L. The NADPH Oxidase Family and Its Inhibitors. Antioxid Redox Signal. 2020 Aug 10;33(5):332-353. doi: 10.1089/ars.2019.7915. Epub 2020 Jan 23. PMID: 31826639. 3: Dorotea D, Kwon G, Lee JH, Saunders E, Bae YS, Moon SH, Lee SJ, Cha DR, Ha H. A pan-NADPH Oxidase Inhibitor Ameliorates Kidney Injury in Type 1 Diabetic Rats. Pharmacology. 2018;102(3-4):180-189. doi: 10.1159/000491398. Epub 2018 Aug 10. PMID: 30099457. 4: Kwon G, Uddin MJ, Lee G, Jiang S, Cho A, Lee JH, Lee SR, Bae YS, Moon SH, Lee SJ, Cha DR, Ha H. A novel pan-Nox inhibitor, APX-115, protects kidney injury in streptozotocin-induced diabetic mice: possible role of peroxisomal and mitochondrial biogenesis. Oncotarget. 2017 Jun 16;8(43):74217-74232. doi: 10.18632/oncotarget.18540. PMID: 29088780; PMCID: PMC5650335. 5: Cha JJ, Min HS, Kim KT, Kim JE, Ghee JY, Kim HW, Lee JE, Han JY, Lee G, Ha HJ, Bae YS, Lee SR, Moon SH, Lee SC, Kim G, Kang YS, Cha DR. APX-115, a first- in-class pan-NADPH oxidase (Nox) inhibitor, protects db/db mice from renal injury. Lab Invest. 2017 Apr;97(4):419-431. doi: 10.1038/labinvest.2017.2. Epub 2017 Feb 6. PMID: 28165467.