[CAS NO. 188791-09-5] JTE-607

Name: JTE-607
Brand: Arctom Scientific
SKU: AS954352

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PRODUCTS SPECIFICATIONS [188791-09-5]

Distributor

Catalog

AS954352

Brand

Arctom Scientific

CAS

188791-09-5

DESCRIPTION [188791-09-5]

Overview

MDL	-
Molecular Weight	597.36
Molecular Formula	C25H33Cl4N3O5
SMILES	CCOC([C@H](CC1=CC=CC=C1)NC(C2=C(C(Cl)=C(C(Cl)=C2)OCCN3CCN(CC3)C)O)=O)=O.Cl.Cl

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

Summary

JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α , IL-1β , IL-6 , IL-8 and IL-10 , from LPS-stimulated human PBMCs, with IC ₅₀ s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively ^[1] . Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607 ^[2] .

In Vitro

JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC ₅₀ s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. The inhibitory effects of JTE-607 are also seen in mRNA expression of those cytokines ^[1] .
JTE-607 inhibits inflammatory cytokine production from LPS-stimulated human PBMCs with an IC ₅₀ of approximately 10 nM ^[1] .
JTE607 inhibits LPS-stimulated IL-8 production from monkey and rabbit PBMCs, and TNF-α production from mouse and rat PBMCs with IC ₅₀ s of 59, 780, 1600 and 19000 nM, respectively ^[1] .
JTE607 also suppresses other cytokines, granulocyte-macrophage colony stimulating factor and IL-1RA with IC ₅₀ s of 2.4±0.8 and 5.4±0.4 nM, respectively ^[1] .
JTE-607 inhibits cytokine production in monkey, rabbit, mouse and rat with IC ₅₀ s of 59±26, 780±120, 1600±650 and 19000±3200 nM, respectively ^[1] .

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

RT-PCR ^[1]

Cell Line:	human peripheral blood mononuclear cells (PBMCs)
Concentration:	100 nM
Incubation Time:	20 hours
Result:	Reduced the increase in the level of mRNAs of TNF-α, IL-1b, IL-6 and IL-8.

In Vivo

JTE-607 (0.3-10 mg/kg, i.v.) shows dose dependent inhibition of mortality after LPS challenge in C. parvum sensitized mice in accordance with a decrease of plasma TNF-α ^[1] .

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

Animal Model:	Male C57BL/6 mice (5 to 6 weeks old) are sensitized by injecting Corynebacterium parvum ^[1]
Dosage:	0.3, 1, 3, 10 mg/kg
Administration:	Administered intravenously 10 min before the LPS challenge.
Result:	Showed dose dependent inhibition of the mortality at 0.3 to 10 mg/kg and significant effect at 3 and 10 mg/kg.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL ( 418.51 mM ; Need ultrasonic)

H ₂ O : 20 mg/mL ( 33.48 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6740 mL	8.3702 mL	16.7403 mL
5 mM	0.3348 mL	1.6740 mL	3.3481 mL
10 mM	0.1674 mL	0.8370 mL	1.6740 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 100 mg/mL (167.40 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.48 mM); Clear solution

* All of the co-solvents are available by MCE.