[CAS NO. 1801185-08-9] SR12418

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PRODUCTS SPECIFICATIONS [1801185-08-9]

Catalog

HY-148103

Brand

MCE

CAS

1801185-08-9

DESCRIPTION [1801185-08-9]

Overview

MDL	-
Molecular Weight	483.57
Molecular Formula	C31H30FNO3
SMILES	O=C(N1CC2=C(C=C(F)C=C2)C[C@H]1COC3=CC=C(OC(C)(C)C)C=C3)C4=C5C=CC=CC5=CC=C4

For research use only. We do not sell to patients.

Summary

SR12418 is a REV-ERB-specific synthetic ligand with IC ₅₀ s of 68 nM and 119 nM for REV-ERBα and REV-ERBβ, respectively. SR12418 can be used in experimental autoimmune encephalomyelitis (EAE) and colitis research ^[1] ^[2] .

IC50 & Target

IC50: 68 nM (REV-ERBα) and 119 nM (REV-ERBβ) ^[1]

In Vitro

SR12418 (5 μM; 96 h) inhibits the growth of TH17 cells ^[1] .
SR12418 (5 and 10 μM; 4 d) inhibits cell differentiation under TH17 polarizing conditions ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR ^[1]

Cell Line:	TH17 cells
Concentration:	5 μM
Incubation Time:	96 hours
Result:	Repressed TH17-mediated gene expression and Nfil3 .

Cell Differentiation Assay ^[1]

Cell Line:	Mouse CD4 ⁺ T cells
Concentration:	5 and 10 μM
Incubation Time:	4 days
Result:	Inhibited TH17 cell differentiation in a dose-dependent manner.

In Vivo

SR12418 (intraperitoneal injection; 50 mg/kg; twice a day) suppresses the development and severity of experimental autoimmune encephalomyelitis ^[1] .
SR12418 (intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization) shows effects in intervention studies of relapsing-remitting experimental autoimmune encephalomyelitis ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 mice inducing experimental autoimmune encephalomyelitis (EAE) ^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; 50 mg/kg; twice a day
Result:	Diminished the incidence of disease with approximately 20% mice developing disease. Showed no overt signs of toxicity.

Animal Model:	PLP139-151-induced relapsing-remitting EAE (R-EAE) in SJL/J mice ^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; 50 mg/kg; twice a day; begin at day 18 post-immunization
Result:	Resulted in a significant reduction in the relapse severity compared to the vehicle control. Showed a significant decrease in the frequency and number of CD4 ⁺ and CD8 ⁺ effector cells (CD44 ^hi ).

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Please store the product under the recommended conditions in the Certificate of Analysis.