RORγt Inverse agonist 6

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RORγt Inverse agonist 6 manufacturers

RORγt Inverse agonist 6 Basic information
Product Name:RORγt Inverse agonist 6
Synonyms:RORγt Inverse agonist 6;Inhibitor,ROR,RORγt Inverse agonist-6,inhibit,RAR-related orphan receptor,RORγt Inverse agonist 6,RORγt Inverse agonist6;2,4-Morpholinedicarboxamide, N2-(3-chloro-4-cyanophenyl)-N4-[3-(cyclopropylmethyl)-1,2,3,4-tetrahydro-1-(1-methylethyl)-2,4-dioxo-6-quinazolinyl]-, (2R)-;RORγt Inverse agonist 6, 10 mM in DMSO;RORγt Inverse agonist 6
CAS:1887161-80-9
MF:C28H29ClN6O5
MW:565.02
EINECS:
Product Categories:
Mol File:1887161-80-9.mol
RORγt Inverse agonist 6 Structure
RORγt Inverse agonist 6 Chemical Properties
density 1.46±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : 50 mg/mL (88.49 mM; Need ultrasonic)
pka11.82±0.70(Predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
RORγt Inverse agonist 6 Usage And Synthesis
UsesRORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo[1].
Biological ActivityRORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo[1]. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in a mouse pharmacodynamics model[1].RORγt Inverse agonist 6 (compound 43) exhibits improved drug exposure (mouse AUC: 1289 ngh/mL at 1 mg/kg, po)[1].RORγt Inverse agonist 6 (compound 43, 30 mg/kg, po, b.i.d) inhibits the expression level of IL-17A by 59% compared to the vehicle after the oral administration at the tested dose[1].
in vivo

RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in a mouse pharmacodynamics model[1].
RORγt Inverse agonist 6 (compound 43) exhibits improved drug exposure (mouse AUC: 1289 ngh/mL at 1 mg/kg, po)[1].
RORγt Inverse agonist 6 (compound 43, 30 mg/kg, po, b.i.d) inhibits the expression level of IL-17A by 59% compared to the vehicle after the oral administration at the tested dose[1].

Animal Model:Mice[1].
Dosage:30 mg/kg.
Administration:Orally twice: at 30 min before and 8 h after IL-23 administration.
Result:Inhibited the expression level of IL-17A by 59% compared to the vehicle after the oral administration at the tested dose.
References[1]. Sato A, et al. Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists. ChemMedChem. 2019 Oct 28.
RORγt Inverse agonist 6 Preparation Products And Raw materials
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