MedKoo Cat#: 555284 | Name: JNJ-55511118
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Description:

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

JNJ-55511118 is a high affinity and selective negative modulator of AMPA receptors containing TARP-γ8 (Ki = 26 nM). JNJ-55511118 had excellent pharmacokinetic properties and achieved high receptor occupancy following oral administration. JNJ-55511118 showed strong, dose-dependent inhibition of neurotransmission within the hippocampus, and a strong anticonvulsant effect.

Chemical Structure

JNJ-55511118
JNJ-55511118
CAS#2036081-86-2

Theoretical Analysis

MedKoo Cat#: 555284

Name: JNJ-55511118

CAS#: 2036081-86-2

Chemical Formula: C14H8ClF3N2O2

Exact Mass: 328.0226

Molecular Weight: 328.68

Elemental Analysis: C, 51.16; H, 2.45; Cl, 10.79; F, 17.34; N, 8.52; O, 9.74

Price and Availability

Size Price Availability Quantity
10mg USD 320.00
50mg USD 910.00
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Related CAS #
No Data
Synonym
JNJ-55511118; JNJ 55511118; JNJ55511118
IUPAC/Chemical Name
5-[2-Chloro-6-(trifluoromethoxy)phenyl]-1,3-dihydro-2H-benzimidazol-2-one
InChi Key
COBXSLRIXGQVGS-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H8ClF3N2O2/c15-8-2-1-3-11(22-14(16,17)18)12(8)7-4-5-9-10(6-7)20-13(21)19-9/h1-6H,(H2,19,20,21)
SMILES Code
O=C1NC2=CC(C3=C(OC(F)(F)F)C=CC=C3Cl)=CC=C2N1
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
2934.99.03.00
More Info
At high levels of receptor occupancy in rodent in vivo models, JNJ-55511118 showed a strong reduction in certain bands on electroencephalogram, transient hyperlocomotion, no motor impairment on rotarod, and a mild impairment in learning and memory. JNJ-55511118 is a novel tool for reversible AMPA receptor inhibition, particularly within the hippocampus, with potential therapeutic utility as an anticonvulsant or neuroprotectant.
Product Data
Biological target:
High affinity and selective negative modulator of AMPA receptors containing TARP-γ8.
In vitro activity:
TBD
In vivo activity:
Oral administration of JNJ-55511118 significantly reduced alcohol-reinforced responding in male mice (Figure 3A–E). Reference: Alcohol Clin Exp Res. 2021 Jul;45(7):1424-1435. https://pubmed.ncbi.nlm.nih.gov/34086361/
Solvent mg/mL mM
Solubility
DMSO 32.9 100.00
Ethanol 32.9 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 328.68 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
Formulation protocol:
1. Hoffman JL, Faccidomo S, Saunders BL, Taylor SM, Kim M, Hodge CW. Inhibition of AMPA receptors (AMPARs) containing transmembrane AMPAR regulatory protein γ-8 with JNJ-55511118 shows preclinical efficacy in reducing chronic repetitive alcohol self-administration. Alcohol Clin Exp Res. 2021 Jul;45(7):1424-1435. doi: 10.1111/acer.14639. Epub 2021 Jun 22. PMID: 34086361; PMCID: PMC8336716. 2. Maher MP, Wu N, Ravula S, Ameriks MK, Savall BM, Liu C, Lord B, Wyatt RM, Matta JA, Dugovic C, Yun S, Ver Donck L, Steckler T, Wickenden AD, Carruthers NI, Lovenberg TW. Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8. J Pharmacol Exp Ther. 2016 May;357(2):394-414. doi: 10.1124/jpet.115.231712. Epub 2016 Mar 17. PMID: 26989142.
In vitro protocol:
TBD
In vivo protocol:
1. Hoffman JL, Faccidomo S, Saunders BL, Taylor SM, Kim M, Hodge CW. Inhibition of AMPA receptors (AMPARs) containing transmembrane AMPAR regulatory protein γ-8 with JNJ-55511118 shows preclinical efficacy in reducing chronic repetitive alcohol self-administration. Alcohol Clin Exp Res. 2021 Jul;45(7):1424-1435. doi: 10.1111/acer.14639. Epub 2021 Jun 22. PMID: 34086361; PMCID: PMC8336716. 2. Maher MP, Wu N, Ravula S, Ameriks MK, Savall BM, Liu C, Lord B, Wyatt RM, Matta JA, Dugovic C, Yun S, Ver Donck L, Steckler T, Wickenden AD, Carruthers NI, Lovenberg TW. Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8. J Pharmacol Exp Ther. 2016 May;357(2):394-414. doi: 10.1124/jpet.115.231712. Epub 2016 Mar 17. PMID: 26989142.
1: Maher MP, Wu N, Ravula S, Ameriks MK, Savall BM, Liu C, Lord B, Wyatt RM, Matta JA, Dugovic C, Yun S, Ver Donck L, Steckler T, Wickenden AD, Carruthers NI, Lovenberg TW. Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8. J Pharmacol Exp Ther. 2016 May;357(2):394-414. doi: 10.1124/jpet.115.231712. Epub 2016 Mar 17. PubMed PMID: 26989142.