JNJ-27141491
Based on 1 Customer Validation
JNJ-27141491 is a selective, noncompetitive and orally active functional antagonist of human CCR2.
For research use only. We do not sell to patients.
- Purity: 97.01%
- CAS No.: 871313-59-6
- Formula: C17H15F2N3O3S
- Molecular Weight:379.38
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hCCR2 |
JNJ-27141491 inhibits MCP-1-induced [35S]GTPγS binding to hCCR2-CHO cell membranes (IC50=38±9 nM) and reduces MCP-1-induced Ca2+ mobilization in hCCR2-CHO cells (IC50=13±1 nM), in THP-1 cells (IC50=13±2 nM), and in human blood monocytes (IC50=43±4 nM). JNJ-27141491 also inhibits chemotaxis of human PBMC toward MCP-1, with an IC50 value of 97±16 nM[1].
JNJ-27141491 competes with the binding of MCP-1 to hCCR2 and acts as a noncompetitive antagonist of the CCR2 receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
JNJ-27141491 (20 mg/kg; oral; daily for 16 days) delays experimental autoimmune encephalomyelitis (EAE) in transgenic CCR2 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Transgenic mCCR2 knockout/hCCR2 knockin C57BL/6 mice[1]
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Dosage:5, 10, 20, or 40 mg/kg
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Administration:Oral, once or twice daily
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Result:Once-daily oral treatment with 40, 20, 10, or 5 mg/kg inhibited the monocyte influx with 77, 57, 49, and 27%, respectively, compared with vehicle treatment, whereas this value was 74 and 22% after twice-daily oral treatment with 20 or 5 mg/kg. The neutrophil influx was also reduced; neutrophil numbers were decreased, with 56, 45, 20, and 8% after 40, 20, 10, or 5 mg/kg q.d. treatments and with 45 and 20% after 20 and 5 mg/kg b.i.d. treatments.
Chemical Information
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CAS No. 871313-59-6
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Appearance Solid
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Molecular Weight 379.38
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Formula C17H15F2N3O3S
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Color Light yellow to yellow
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SMILES
CC[C@@H](C1=CC(F)=C(F)C=C1)N2C(C(OC)=O)=C(C3=CC=NO3)NC2=S
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 50 mg/mL (131.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Buntinx M, et al. Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor CCR2. J Pharmacol Exp Ther. 2008 Oct;327(1):1-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6359 mL | 13.1794 mL | 26.3588 mL | 65.8970 mL |
| 5 mM | 0.5272 mL | 2.6359 mL | 5.2718 mL | 13.1794 mL | |
| 10 mM | 0.2636 mL | 1.3179 mL | 2.6359 mL | 6.5897 mL | |
| 15 mM | 0.1757 mL | 0.8786 mL | 1.7573 mL | 4.3931 mL | |
| 20 mM | 0.1318 mL | 0.6590 mL | 1.3179 mL | 3.2948 mL | |
| 25 mM | 0.1054 mL | 0.5272 mL | 1.0544 mL | 2.6359 mL | |
| 30 mM | 0.0879 mL | 0.4393 mL | 0.8786 mL | 2.1966 mL | |
| 40 mM | 0.0659 mL | 0.3295 mL | 0.6590 mL | 1.6474 mL | |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5272 mL | 1.3179 mL | |
| 60 mM | 0.0439 mL | 0.2197 mL | 0.4393 mL | 1.0983 mL | |
| 80 mM | 0.0329 mL | 0.1647 mL | 0.3295 mL | 0.8237 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6590 mL |
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