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MedKoo Cat#: 529212 | Name: Obefazimod
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Description:

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

Obefazimod, also known as SPL-464 and ABX-464, is a quinoline derivative and an inhibitor of the HIV replication potentially for the treatment of HIV infection. Obefazimod upregulates a single microRNA (miR-124) in immune cells and reduces the production of various inflammatory cytokines and chemokines.

Chemical Structure

Obefazimod
Obefazimod
CAS#1258453-75-6

Theoretical Analysis

MedKoo Cat#: 529212

Name: Obefazimod

CAS#: 1258453-75-6

Chemical Formula: C16H10ClF3N2O

Exact Mass: 338.0434

Molecular Weight: 338.71

Elemental Analysis: C, 56.74; H, 2.98; Cl, 10.47; F, 16.83; N, 8.27; O, 4.72

Price and Availability

Size Price Availability Quantity
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
200mg USD 2,150.00 2 Weeks
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Related CAS #
No Data
Synonym
Obefazimod; ABX-464; ABX 464; ABX464; SPL-464; SPL 464; SPL464;
IUPAC/Chemical Name
8-chloro-N-(4-(trifluoromethoxy)phenyl)quinolin-2-amine
InChi Key
OZOGDCZJYVSUBR-UHFFFAOYSA-N
InChi Code
InChI=1S/C16H10ClF3N2O/c17-13-3-1-2-10-4-9-14(22-15(10)13)21-11-5-7-12(8-6-11)23-16(18,19)20/h1-9H,(H,21,22)
SMILES Code
FC(F)(F)OC1=CC=C(NC2=NC3=C(Cl)C=CC=C3C=C2)C=C1
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

Preparing Stock Solutions

The following data is based on the product molecular weight 338.71 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: Pai S, Mudgal J, Kamath BV, Pai KSR. An insight on promising strategies hoping to cure HIV-1 infection by targeting Rev protein-short review. Pharmacol Rep. 2021 Apr 11. doi: 10.1007/s43440-021-00257-9. Epub ahead of print. PMID: 33840054. 2: Vermeire S, Hébuterne X, Tilg H, De Hertogh G, Gineste P, Steens JM; ABX464 Investigators. Induction and Long-term Follow-up With ABX464 for Moderate-to- severe Ulcerative Colitis: Results of Phase IIa Trial. Gastroenterology. 2021 Jun;160(7):2595-2598.e3. doi: 10.1053/j.gastro.2021.02.054. Epub 2021 Mar 2. PMID: 33662385. 3: Tazi J, Begon-Pescia C, Campos N, Apolit C, Garcel A, Scherrer D. Specific and selective induction of miR-124 in immune cells by the quinoline ABX464: a transformative therapy for inflammatory diseases. Drug Discov Today. 2021 Apr;26(4):1030-1039. doi: 10.1016/j.drudis.2020.12.019. Epub 2020 Dec 30. PMID: 33387693. 4: Rutsaert S, Steens JM, Gineste P, Cole B, Kint S, Barrett PN, Tazi J, Scherrer D, Ehrlich HJ, Vandekerckhove L. Safety, tolerability and impact on viral reservoirs of the addition to antiretroviral therapy of ABX464, an investigational antiviral drug, in individuals living with HIV-1: a Phase IIa randomised controlled study. J Virus Erad. 2019 Jan 1;5(1):10-22. PMID: 30800421; PMCID: PMC6362909. 5: Vautrin A, Manchon L, Garcel A, Campos N, Lapasset L, Laaref AM, Bruno R, Gislard M, Dubois E, Scherrer D, Ehrlich JH, Tazi J. Both anti-inflammatory and antiviral properties of novel drug candidate ABX464 are mediated by modulation of RNA splicing. Sci Rep. 2019 Jan 28;9(1):792. doi: 10.1038/s41598-018-37813-y. PMID: 30692590; PMCID: PMC6349857. 6: Manchon L, Chebli K, Papon L, Paul C, Garcel A, Campos N, Scherrer D, Ehrlich H, Hahne M, Tazi J. RNA sequencing analysis of activated macrophages treated with the anti-HIV ABX464 in intestinal inflammation. Sci Data. 2017 Oct 17;4:170150. doi: 10.1038/sdata.2017.150. PMID: 29039845; PMCID: PMC5644369. 7: Chebli K, Papon L, Paul C, Garcel A, Campos N, Scherrer D, J Ehrlich H, Hahne M, Tazi J. The Anti-Hiv Candidate Abx464 Dampens Intestinal Inflammation by Triggering Il-22 Production in Activated Macrophages. Sci Rep. 2017 Jul 7;7(1):4860. doi: 10.1038/s41598-017-04071-3. PMID: 28687795; PMCID: PMC5501810. 8: Steens JM, Scherrer D, Gineste P, Barrett PN, Khuanchai S, Winai R, Ruxrungtham K, Tazi J, Murphy R, Ehrlich H. Safety, Pharmacokinetics, and Antiviral Activity of a Novel HIV Antiviral, ABX464, in Treatment-Naive HIV- Infected Subjects in a Phase 2 Randomized, Controlled Study. Antimicrob Agents Chemother. 2017 Jun 27;61(7):e00545-17. doi: 10.1128/AAC.00545-17. PMID: 28507108; PMCID: PMC5487684. 9: Scherrer D, Rouzier R, Noel Barrett P, Steens JM, Gineste P, Murphy RL, Tazi J, Ehrlich HJ. Pharmacokinetics and tolerability of ABX464, a novel first-in- class compound to treat HIV infection, in healthy HIV-uninfected subjects. J Antimicrob Chemother. 2017 Mar 1;72(3):820-828. doi: 10.1093/jac/dkw458. PMID: 27999038. 10: Scherrer D, Rouzier R, Cardona M, Barrett PN, Steens JM, Gineste P, Murphy RL, Tazi J, Ehrlich HJ. Randomized Trial of Food Effect on Pharmacokinetic Parameters of ABX464 Administered Orally to Healthy Male Subjects. Antimicrob Agents Chemother. 2016 Dec 27;61(1):e01288-16. doi: 10.1128/AAC.01288-16. PMID: 27799203; PMCID: PMC5192114. 11: Berkhout B, van der Velden YU. ABX464: a good drug candidate instead of a magic bullet. Retrovirology. 2015 Jul 28;12:64. doi: 10.1186/s12977-015-0189-x. PMID: 26215448; PMCID: PMC4515925. 12: Campos N, Myburgh R, Garcel A, Vautrin A, Lapasset L, Nadal ES, Mahuteau- Betzer F, Najman R, Fornarelli P, Tantale K, Basyuk E, Séveno M, Venables JP, Pau B, Bertrand E, Wainberg MA, Speck RF, Scherrer D, Tazi J. Long lasting control of viral rebound with a new drug ABX464 targeting Rev - mediated viral RNA biogenesis. Retrovirology. 2015 Apr 9;12:30. doi: 10.1186/s12977-015-0159-3. PMID: 25889234; PMCID: PMC4422473.

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