JNJ-10397049

Cat. No.: HY-10896 Purity: 99.91%: FAQs
Data Sheet SDS COA Handling Instructions

JNJ-10397049 is a potent and selective orexin 2 receptor (OX₂R) antagonist, with a pK_i of 8.3. JNJ-10397049 is 600-fold selective for the OX₂R over the OX₁R.

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

JNJ-10397049 Chemical Structure

CAS No. : 708275-58-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solution
10 mM * 1 mL in DMSO	USD 141	In-stock	Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL ready for reconstitution	USD 141	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 440	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 770	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1155	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

JNJ-10397049 is a potent and selective orexin 2 receptor (OX₂R) antagonist, with a pK_i of 8.3. JNJ-10397049 is 600-fold selective for the OX₂R over the OX₁R^[1]^[2].

In Vivo

JNJ-10397049 (10-30 mg/kg) decreases the latency for persistent sleep and increased nonrapid eye movement and rapid eye movement sleep time^[2].
JNJ-10397049 blocks ethanol self-administration, place preference and reinstatement^[3].

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

Animal Model:	Male Sprague-Dawley rats^[2].
Dosage:	10 mg/kg.
Administration:	Subcutaneous administration.
Result:	Induced a significant reduction in NREM sleep latency and an increase in NREM sleep duration during the first 2 h after administration relative to vehicle treatment.

Molecular Weight

484.18

Appearance

Solid

Formula

C₁₉H₂₀Br₂N₂O₃

CAS No.

708275-58-5

SMILES

BrC1=C(NC(N[C@@H]2[C@H](C3=CC=CC=C3)OC(C)(C)OC2)=O)C=CC(Br)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 170 mg/mL (351.11 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0653 mL	10.3267 mL	20.6535 mL
5 mM	0.4131 mL	2.0653 mL	4.1307 mL
10 mM	0.2065 mL	1.0327 mL	2.0653 mL

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

In Vivo:

1.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 4.25 mg/mL (8.78 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 4.25 mg/mL (8.78 mM); Clear solution

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

Purity & Documentation

Purity: 99.91%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (250 KB) HNMR (261 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Laura C McAtee, et al. Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4225-9. [Content Brief]

[2]. Christine Dugovic, et al. Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat. J Pharmacol Exp Ther. 2009 Jul;330(1):142-51. [Content Brief]

[3]. Da-Thao Tran, et al. Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists. Eur J Pharmacol. 2011 Sep 30;667(1-3):120-8. [Content Brief]

JNJ-10397049 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

JNJ-10397049708275-58-5JNJ10397049JNJ 10397049Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorNREMsleeplatencyInhibitorinhibitorinhibit

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JNJ-10397049

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