2(1H)-Isoquinolinecarboxamide, N-(4-fluorophenyl)-3,4-dihydro-1-[4-(trifluoromethyl)phenyl]-, (1R)- manufacturers
- AMG8788
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- $2140.00
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2026-04-20
- CAS:1159996-43-6
- Purity:
- Supply Ability: 10g
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| | 2(1H)-Isoquinolinecarboxamide, N-(4-fluorophenyl)-3,4-dihydro-1-[4-(trifluoromethyl)phenyl]-, (1R)- Basic information |
| | 2(1H)-Isoquinolinecarboxamide, N-(4-fluorophenyl)-3,4-dihydro-1-[4-(trifluoromethyl)phenyl]-, (1R)- Chemical Properties |
| Boiling point | 555.4±50.0 °C(Predicted) | | density | 1.346±0.06 g/cm3(Predicted) | | pka | 11.60±0.70(Predicted) |
| | 2(1H)-Isoquinolinecarboxamide, N-(4-fluorophenyl)-3,4-dihydro-1-[4-(trifluoromethyl)phenyl]-, (1R)- Usage And Synthesis |
| Uses | AMG8788 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 63.2 nM[1]. | | in vivo | AMG8788 (30 mg/kg; p.o.; once) elicits a transient decrease in body temperature (Tb) in rats[1]. | Animal Model: | Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age) [1] | | Dosage: | 30 mg/kg | | Administration: | Oral administration, once | | Result: | Produced a significant decrease of Tb from 40 min to 70 min post dosing.
Effect of AMG8788 on Tb in rats. P value is for comparing compound administered rat Tb with vehicle administered rat Tb. End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCT
| Compound | Dose mg/kg (route) | Max Tb decrease (°C) | P value * | Time post dosing (min) | Plasma concentration | | AMG8788 | 30 (p.o.) | 0.53 | p < 0.05 | 40 | 1.5 ± 0.6 |
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| | IC 50 | TRPM8: 63.2 nM (IC50); TRPA1: 1 μM (IC50) | | References | [1] Gavva NR, et al. Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Mol Pain. 2012 May 9;8:36. DOI:10.1186/1744-8069-8-36 |
| | 2(1H)-Isoquinolinecarboxamide, N-(4-fluorophenyl)-3,4-dihydro-1-[4-(trifluoromethyl)phenyl]-, (1R)- Preparation Products And Raw materials |
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