Synonym
Inaxaplin; Inaxapline; Inaxaplina;
IUPAC/Chemical Name
3-(5,7-difluoro-2-(4-fluorophenyl)-1H-indol-3-yl)-N-((3S,4R)-4-hydroxy-2-oxopyrrolidin-3-yl)propanamide
InChi Key
CTXLPYZCBOVVQK-UZLBHIALSA-N
InChi Code
InChI=1S/C21H18F3N3O3/c22-11-3-1-10(2-4-11)18-13(14-7-12(23)8-15(24)19(14)27-18)5-6-17(29)26-20-16(28)9-25-21(20)30/h1-4,7-8,16,20,27-28H,5-6,9H2,(H,25,30)(H,26,29)/t16-,20+/m1/s1
SMILES Code
O=C(N[C@@H]1C(NC[C@H]1O)=O)CCC2=C(C3=CC=C(F)C=C3)NC4=C2C=C(F)C=C4F
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
To be determined
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
417.39
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.
| 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: Egbuna O, Zimmerman B, Manos G, Fortier A, Chirieac MC, Dakin LA, Friedman
DJ, Bramham K, Campbell K, Knebelmann B, Barisoni L, Falk RJ, Gipson DS,
Lipkowitz MS, Ojo A, Bunnage ME, Pollak MR, Altshuler D, Chertow GM;
VX19-147-101 Study Group. Inaxaplin for Proteinuric Kidney Disease in Persons
with Two APOL1 Variants. N Engl J Med. 2023 Mar 16;388(11):969-979. doi:
10.1056/NEJMoa2202396. PMID: 36920755.
2: Egbuna O, Chertow GM. Inaxaplin for Proteinuric Kidney Disease in Persons
with Two APOL1 Variants. Reply. N Engl J Med. 2023 Jun 29;388(26):2491. doi:
10.1056/NEJMc2304780. PMID: 37379148.
3: Gbadegesin R, Lane B. Inaxaplin for the treatment of APOL1-associated kidney
disease. Nat Rev Nephrol. 2023 Aug;19(8):479-480. doi:
10.1038/s41581-023-00721-0. PMID: 37106136; PMCID: PMC10461697.
4: Soler MJ, Glassock RJ, Fervenza FC. Inaxaplin for Proteinuric Kidney Disease
in Persons with Two APOL1 Variants. N Engl J Med. 2023 Jun 29;388(26):2490. doi:
10.1056/NEJMc2304780. PMID: 37379147.
5: Caparali EB, De Gregorio V, Barua M. Genetic Causes of Nephrotic Syndrome and
Focal and Segmental Glomerulosclerosis. Adv Kidney Dis Health. 2024
Jul;31(4):309-316. doi: 10.1053/j.akdh.2024.04.001. PMID: 39084756.
6: Egbuna O, Audard V, Manos G, Tian S, Hagos F, Chertow GM. Safety and
Tolerability of the APOL1 Inhibitor, Inaxaplin, following Single- and Multiple-
Ascending Doses in Healthy Adults. Glomerular Dis. 2024 Mar 14;4(1):64-73. doi:
10.1159/000538255. PMID: 38600955; PMCID: PMC11006409.
7: Bonilla M, Efe O, Selvaskandan H, Lerma EV, Wiegley N. A Review of Focal
Segmental Glomerulosclerosis Classification With a Focus on Genetic
Associations. Kidney Med. 2024 Apr 17;6(6):100826. doi:
10.1016/j.xkme.2024.100826. PMID: 38765809; PMCID: PMC11099322.
