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MedKoo Cat#: 574265 | Name: Bersacapavir
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Description:

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

Bersacapavir, also known as JNJ-6379, JNJ-56136379, or JNJ-379, a capsid assembly modulator that blocks hepatitis B virus (HBV) replication. JNJ-56136379 median 50% effective concentration (EC50) values across all genotypes were 10-33 nM versus 17 nM (genotype D reference). JNJ-56136379 remained active against isolates carrying nucleos(t)ide analogue resistance mutations (median EC50 2-25 nM) or basal core promoter (BCP) ± precore (PC) mutations (median EC50 13-20 nM) or PC mutations (median EC50 11 nM), representing activity against isolates from HBeAg-positive and -negative hepatitis B patients.

Chemical Structure

Bersacapavir
Bersacapavir
CAS#1638266-40-6 (free)

Theoretical Analysis

MedKoo Cat#: 574265

Name: Bersacapavir

CAS#: 1638266-40-6 (free)

Chemical Formula: C16H14F4N4O3S

Exact Mass: 418.0723

Molecular Weight: 418.37

Elemental Analysis: C, 45.93; H, 3.37; F, 18.16; N, 13.39; O, 11.47; S, 7.66

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
1g USD 4,650.00 2 Weeks
2g USD 6,950.00 2 Weeks
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Related CAS #
1638266-40-6 (free) Bersacapavir hydrate
Synonym
JNJ-6379; JNJ 6379; JNJ6379; JNJ-56136379; JNJ 56136379; JNJ56136379; JNJ-379; JNJ 379; JNJ379; Bersacapavir;
IUPAC/Chemical Name
N-(3-cyano-4-fluorophenyl)-1-methyl-4-{[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl}-1H-pyrrole-2-carboxamide
InChi Key
SBVBIDUKSBJYEF-VIFPVBQESA-N
InChi Code
InChI=1S/C16H14F4N4O3S/c1-9(16(18,19)20)23-28(26,27)12-6-14(24(2)8-12)15(25)22-11-3-4-13(17)10(5-11)7-21/h3-6,8-9,23H,1-2H3,(H,22,25)/t9-/m0/s1
SMILES Code
O=C(C1=CC(S(=O)(N[C@@H](C)C(F)(F)F)=O)=CN1C)NC2=CC=C(F)C(C#N)=C2
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

Preparing Stock Solutions

The following data is based on the product molecular weight 418.37 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: Yuen MF, Locarnini S, Lim TH, Strasser SI, Sievert W, Cheng W, Thompson AJ, Given BD, Schluep T, Hamilton J, Biermer M, Kalmeijer R, Beumont M, Lenz O, De Ridder F, Cloherty G, Ka-Ho Wong D, Schwabe C, Jackson K, Lai CL, Gish RG, Gane E. Combination treatments including the small-interfering RNA JNJ-3989 induce rapid and sometimes prolonged viral responses in patients with CHB. J Hepatol. 2022 Nov;77(5):1287-1298. doi: 10.1016/j.jhep.2022.07.010. Epub 2022 Jul 20. PMID: 35870702. 2: Vandenbossche J, Jessner W, van den Boer M, Biewenga J, Berke JM, Talloen W, De Zwart L, Snoeys J, Yogaratnam J. Pharmacokinetics, Safety and Tolerability of JNJ-56136379, a Novel Hepatitis B Virus Capsid Assembly Modulator, in Healthy Subjects. Adv Ther. 2019 Sep;36(9):2450-2462. doi: 10.1007/s12325-019-01017-1. Epub 2019 Jul 2. Erratum in: Adv Ther. 2020 Mar 4;: PMID: 31267367. 3: Zoulim F, Lenz O, Vandenbossche JJ, Talloen W, Verbinnen T, Moscalu I, Streinu-Cercel A, Bourgeois S, Buti M, Crespo J, Manuel Pascasio J, Sarrazin C, Vanwolleghem T, Shukla U, Fry J, Yogaratnam JZ. JNJ-56136379, an HBV Capsid Assembly Modulator, Is Well-Tolerated and Has Antiviral Activity in a Phase 1 Study of Patients With Chronic Infection. Gastroenterology. 2020 Aug;159(2):521-533.e9. doi: 10.1053/j.gastro.2020.04.036. Epub 2020 Apr 25. PMID: 32343960. 4: Berke JM, Dehertogh P, Vergauwen K, Mostmans W, Vandyck K, Raboisson P, Pauwels F. Antiviral Properties and Mechanism of Action Studies of the Hepatitis B Virus Capsid Assembly Modulator JNJ-56136379. Antimicrob Agents Chemother. 2020 Apr 21;64(5):e02439-19. doi: 10.1128/AAC.02439-19. PMID: 32094138; PMCID: PMC7179615. 5: Verbinnen T, Hodari M, Talloen W, Berke JM, Blue D, Yogaratnam J, Vandenbossche J, Shukla U, De Meyer S, Lenz O. Virology analysis of chronic hepatitis B virus-infected patients treated for 28 days with JNJ-56136379 monotherapy. J Viral Hepat. 2020 Nov;27(11):1127-1137. doi: 10.1111/jvh.13351. Epub 2020 Jul 20. PMID: 32579776. 6: Soriano V, Barreiro P, Cachay E, Kottilil S, Fernandez-Montero JV, de Mendoza C. Advances in hepatitis B therapeutics. Ther Adv Infect Dis. 2020 Oct 15;7:2049936120965027. doi: 10.1177/2049936120965027. PMID: 33117536; PMCID: PMC7570774. 7: Kakuda TN, Halabi A, Klein G, Sanga M, Guinard-Azadian C, Kowalik M, Nedoschinsky K, Nangosyah J, Ediage EN, Hillewaert V, Verboven P, Goris I, Snoeys J, Palmer M, Biermer M. Pharmacokinetics of JNJ-73763989 and JNJ-56136379 (Bersacapavir) in Participants With Moderate Hepatic Impairment. J Clin Pharmacol. 2023 Jun;63(6):732-741. doi: 10.1002/jcph.2214. Epub 2023 Mar 20. PMID: 36786053. 8: Gane E, Yuen MF, Kakuda TN, Ogawa T, Takahashi Y, Goeyvaerts N, Lonjon- Domanec I, Vaughan T, Schluep T, Hamilton J, Njumbe Ediage E, Hillewaert V, Snoeys J, Lenz O, Talloen W, Biermer M. JNJ-73763989 pharmacokinetics and safety: Liver-targeted siRNAs against hepatitis B virus, in Japanese and non- Japanese healthy adults, and combined with JNJ-56136379 and a nucleos(t)ide analogue in patients with chronic hepatitis B. Antivir Ther. 2022 Jun;27(3):13596535221093856. doi: 10.1177/13596535221093856. PMID: 35695169. 9: Vandenbossche J, Yogaratnam J, Hillewaert V, Rasschaert F, Talloen W, Biewenga J, Snoeys J, Kakuda TN, Palmer M, Nangosyah J, Biermer M. Drug-Drug Interactions With the Hepatitis B Virus Capsid Assembly Modulator JNJ-56136379 (Bersacapavir). Clin Pharmacol Drug Dev. 2022 Dec;11(12):1419-1429. doi: 10.1002/cpdd.1164. Epub 2022 Sep 5. PMID: 36062869; PMCID: PMC10087559. 10: Smolders EJ, Burger DM, Feld JJ, Kiser JJ. Review article: clinical pharmacology of current and investigational hepatitis B virus therapies. Aliment Pharmacol Ther. 2020 Jan;51(2):231-243. doi: 10.1111/apt.15581. Epub 2019 Dec 16. PMID: 31840863. 11: Verbinnen T, Tan Y, Wang G, Dehertogh P, Vergauwen K, Neefs JM, Jacoby E, Lenz O, Berke JM. Anti-HBV activity of the HBV capsid assembly modulator JNJ-56136379 across full-length genotype A-H clinical isolates and core site- directed mutants in vitro. J Antimicrob Chemother. 2020 Sep 1;75(9):2526-2534. doi: 10.1093/jac/dkaa179. PMID: 32417895. 12: Janssen HLA, Hou J, Asselah T, Chan HLY, Zoulim F, Tanaka Y, Janczewska E, Nahass RG, Bourgeois S, Buti M, Lampertico P, Lenz O, Verbinnen T, Vandenbossche J, Talloen W, Kalmeijer R, Beumont M, Biermer M, Shukla U. Randomised phase 2 study (JADE) of the HBV capsid assembly modulator JNJ-56136379 with or without a nucleos(t)ide analogue in patients with chronic hepatitis B infection. Gut. 2023 Jul;72(7):1385-1398. doi: 10.1136/gutjnl-2022-328041. Epub 2023 Jan 25. PMID: 36697207. 13: Vandenbossche J, Jessner W, van den Boer M, Biewenga J, Berke JM, Talloen W, De Zwart L, Snoeys J, Vandyck K, Fry J, Yogaratnam J. Correction to: Pharmacokinetics, Safety and Tolerability of JNJ-56136379, a Novel Hepatitis B Virus Capsid Assembly Modulator, in Healthy Subjects. Adv Ther. 2020 Apr;37(4):1703. doi: 10.1007/s12325-020-01249-6. Erratum for: Adv Ther. 2019 Sep;36(9):2450-2462. PMID: 32133584. 14: Vermes T, Kielpinski M, Henkel T, Pericàs MA, Alza E, Corcuera A, Buschmann H, Goldner T, Urban A. An automated microfluidic platform for the screening and characterization of novel hepatitis B virus capsid assembly modulators. Anal Methods. 2022 Jan 6;14(2):135-146. doi: 10.1039/d1ay01227d. PMID: 34918017.