1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]-

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1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]- manufacturers
1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]- Basic information
Product Name:1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]-
Synonyms:1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]-
CAS:2815263-05-7
MF:C29H27N5O
MW:461.56
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Mol File:2815263-05-7.mol
1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]- Structure
1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]- Chemical Properties
Boiling point 693.6±65.0 °C(Predicted)
density 1.251±0.06 g/cm3(Predicted)
pka16.13±0.30(Predicted)
form Solid
color Light yellow to yellow
Safety Information
MSDS Information
1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]- Usage And Synthesis
UsesGPR84 antagonist 3 (compound 42) is a potent GPR84 (G-protein-coupled receptor 84) antagonist. GPR84 antagonist 3 inhibits GTPγS, with a pIC50 of 8.28. GPR84 antagonist 3 has a favorable pharmacokinetic profile suitable[1].
in vivo

GPR84 antagonist 3 (compound 42) (1 mg/kg (IV), 10 mg/kg (Orally); once) has a good elimination half-life (2.51 h), moderate rate of clearance, and bioavailability[1].

Animal Model:Male C57BL/6J mice (n = 3)[1]
Dosage:1 mg/kg (IV), 10 mg/kg (Orally)
Administration:IV, Orally; once (Pharmacokinetic Analysis)
Result:Pharmacokinetic Parameters of GPR84 antagonist 3 in Male C57BL/6J mice[1].
IV (1 mg/kg)PO (10 mg/kg)
half-life (h)2.51 ± 6.55
CL (mL/min/kg)38.9 ± 13.9
Vss (L/kg)7.24 ± 9.2
C0 (ng/mL)394 ± 19.1
AUCall (ng/mL·h)420 ± 12.51590 ± 18.7
Tmax (h)1
Cmax (ng/mL)402 ± 31.8
F (%)36.8 ± 18.7
References[1] Mahindra A, et al. Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists. J Med Chem. 2022 Aug 10. DOI:10.1021/acs.jmedchem.2c00804
1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]- Preparation Products And Raw materials
Tag:1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]-(2815263-05-7) Related Product Information
1H-Indole, 3-[[6-[4-(4-morpholinylmethyl)phenyl]-5-phenyl-1,2,4-triazin-3-yl]methyl]- GPR84 antagonist 1 NA 3,3′-Methylenebis[5,7-difluoro-1H-indole] TUG-2099 NA