APX-115 free base
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MedKoo CAT#: 555871

CAS#: 1270084-92-8

Description: 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.


Price and Availability

Size Price Shipping out time Quantity
100mg USD 950 2 Weeks
200mg USD 1850 2 Weeks
500mg USD 2650 2 Weeks
1g USD 3650 2 Weeks
2g USD 5950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-12-02. Prices are subject to change without notice.

APX-115 free base is in stock.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 555871
Name: APX-115 free base
CAS#: 1270084-92-8
Chemical Formula: C17H17N3O
Exact Mass: 279.1372
Molecular Weight: 279.343
Elemental Analysis: C, 73.10; H, 6.13; N, 15.04; O, 5.73


Synonym: APX-115 free base; APX 115; APX115; EWHA-18278; EWHA 18278; EWHA18278;

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


Technical Data

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


Additional Information

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.


References

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.