Nelremagpran
CAS 2492595-24-9
MFC15H9ClF4O3 MW 348.67 g/mol
3-[[2-Chloro-4-(trifluoromethyl)phenoxy]methyl]-2-fluorobenzoic acid
3-{[2-chloro-4-(trifluoromethyl)phenoxy]methyl}-2-fluorobenzoic acid
Mas-related G protein-coupled receptor inverse agonist, anti-inflammatory, MRGPRX4 modulator-2, BL83FAK6DZ,
Nelremagpran is an experimental drug that acts as a potent and selective antagonist (or possibly inverse agonist) of the MAS-related Gq protein-coupled receptor X4 (MRGPRX4). It has antiinflammatory effects in animal studies. This receptor is poorly characterised but is thought to be involved in immune system function, and development of selective ligands is essential for researching its role in the body.[1][2]
Nelremagpran is an experimental drug that acts as a potent and selective antagonist or inverse agonist of the Mas-related G-protein-coupled receptor X4 (MRGPRX4). It was initially developed by Escient Pharmaceuticals, Inc. for its anti-inflammatory and anti-itch properties.
🧪 Core Mechanism
The drug targets MRGPRX4, a poorly characterized receptor found in the immune and nervous systems. It functions with high potency, exhibiting an half-maximal inhibitory concentration (IC50) of less than 100 nM.
🔬 Potential Research Applications
Because the receptor plays a significant role in mediating severe itch and pain pathways, Nelremagpran is actively used as a chemical probe to study:
- Chronic Pruritus: Conditions involving persistent, debilitating itch sensations, such as cholestatic pruritus.
- Autoimmune Diseases: Underlying mechanisms in conditions like psoriasis, multiple sclerosis, and Stevens-Johnson Syndrome.
- Inflammatory Sensation: How the body signals pain and immune hypersensitivity
PAT
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2020198537&_cid=P12-MREAZN-03524-1
Synthesis of Compound 1-55
Step 4-4. Synthesis of methyl 3-(bromomethyl)-2-fluorc>benzoate (INT 4-C)
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References
 | |
| Identifiers | |
|---|---|
| IUPAC name | |
| CAS Number | 2492595-24-9 |
| PubChem CID | 155145968 |
| ChemSpider | 115008493 |
| UNII | BL83FAK6DZ |
| ChEMBL | ChEMBL4855031 |
| Chemical and physical data | |
| Formula | C15H9ClF4O3 |
| Molar mass | 348.68 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
References
- WO 2020/198537, Yeager A, Selfridge B, Sainz M, Martinborough E, Boehm M, Huang, “Modulators of mas-related G-protein receptor x4 and related products and methods.”, published 1 October 2020, assigned to Escient Pharmaceuticals, Inc.
- “International Nonproprietary Names for Pharmaceutical Substances (INN)” (PDF). WHO Drug Information. 38 (4). 2024.
- Modulators of Mas-related G-protein receptor X4 and related products and methodsPublication Number: US-11840521-B2Priority Date: 2019-03-28Grant Date: 2023-12-12
- Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: EP-3946304-A1Priority Date: 2019-03-28
- Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2023159474-A1Priority Date: 2019-03-28
- Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2023053860-A1Priority Date: 2019-03-28
- Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2021032213-A1Priority Date: 2019-03-28
- Modulators of mas-related G-protein receptor X4 and related products and methodsPublication Number: US-11643399-B2Priority Date: 2019-03-28Grant Date: 2023-05-09
- Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: US-2024300907-A1Priority Date: 2019-03-28
- Modulators of mas-related g-protein receptor x4 and related products and methodsPublication Number: WO-2020198537-A1Priority Date: 2019-03-28
- Modulators of MAS-related G protein receptor X4 and related products and methodsPublication Number: CN-113939288-BPriority Date: 2019-03-28Grant Date: 2025-04-25
//////////nelremagpran, anax labs, Mas-related G protein-coupled receptor inverse agonist, anti-inflammatory, MRGPRX4 modulator-2, BL83FAK6DZ,