Synonym
Elsulfavirine sodium; R 1206; R1206; R-1206 sodium; R1206(sodium salt); Elpida
IUPAC/Chemical Name
sodium ((4-(2-(4-bromo-3-(3-chloro-5-cyanophenoxy)-2-fluorophenyl)acetamido)-3-chlorophenyl)sulfonyl)(propionyl)amide
InChi Key
UJFARQSHFFWJHD-UHFFFAOYSA-M
InChi Code
InChI=1S/C24H17BrCl2FN3O5S.Na/c1-2-21(32)31-37(34,35)17-4-6-20(19(27)11-17)30-22(33)9-14-3-5-18(25)24(23(14)28)36-16-8-13(12-29)7-15(26)10-16;/h3-8,10-11H,2,9H2,1H3,(H2,30,31,32,33);/q;+1/p-1
SMILES Code
CCC([N-]S(=O)(C1=CC=C(NC(CC2=CC=C(Br)C(OC3=CC(C#N)=CC(Cl)=C3)=C2F)=O)C(Cl)=C1)=O)=O.[Na+]
Appearance
To be determined
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
651.26
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: Al-Salama ZT. Elsulfavirine: First Global Approval. Drugs. 2017 Oct;77(16):1811-1816. doi: 10.1007/s40265-017-0820-3. PMID: 28940154.
2: Li G, Wang Y, De Clercq E. Approved HIV reverse transcriptase inhibitors in the past decade. Acta Pharm Sin B. 2022 Apr;12(4):1567-1590. doi: 10.1016/j.apsb.2021.11.009. Epub 2021 Nov 16. Erratum in: Acta Pharm Sin B. 2023 Aug;13(8):3581. PMID: 35847492; PMCID: PMC9279714.
3: Supuran CT, Nocentini A, Yakubova E, Savchuk N, Kalinin S, Krasavin M. Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida®) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms. J Enzyme Inhib Med Chem. 2021 Dec;36(1):1056-1060. doi: 10.1080/14756366.2021.1927007. PMID: 34000969; PMCID: PMC8143618.
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5: Wang Y, De Clercq E, Li G. Current and emerging non-nucleoside reverse transcriptase inhibitors (NNRTIs) for HIV-1 treatment. Expert Opin Drug Metab Toxicol. 2019 Oct;15(10):813-829. doi: 10.1080/17425255.2019.1673367. Epub 2019 Oct 17. PMID: 31556749.
6: Singh AK, Kumar A, Arora S, Kumar R, Verma A, Khalilullah H, Jaremko M, Emwas AH, Kumar P. Current insights and molecular docking studies of HIV-1 reverse transcriptase inhibitors. Chem Biol Drug Des. 2023 Oct 10. doi: 10.1111/cbdd.14372. Epub ahead of print. PMID: 37817296.
7: Battini L, Bollini M. Challenges and approaches in the discovery of human immunodeficiency virus type-1 non-nucleoside reverse transcriptase inhibitors. Med Res Rev. 2019 Jul;39(4):1235-1273. doi: 10.1002/med.21544. Epub 2018 Nov 11. PMID: 30417402.
