SB-408124

Cat. No.: HY-70068 Purity: 98.27%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SB-408124 is a non-peptide OX1 receptor antagonist with K_is of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor.

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

SB-408124 Chemical Structure

CAS No. : 288150-92-5

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 75	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 75	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Other Forms of SB-408124:

SB-408124 Hydrochloride In-stock

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OX₂ Receptor OX₁ Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

SB-408124 is a non-peptide OX1 receptor antagonist with K_is of 57 nM and 27 nM in whole cell and membrane, respectively. SB-408124 exhibits 50-fold selectivity over OX2 receptor^[1].

IC₅₀ & Target^[1]

OX₁ Receptor

57 nM (Ki, in whole cell )

OX₁ Receptor

27 nM (Ki, in cell membrane)

In Vivo

SB-408124 (30 μg/10 μl; i.c.v.; male Wistar rats) decreases Orexin-A induced water intake in Wistar rats^[2].

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

Molecular Weight

356.37

Formula

C₁₉H₁₈F₂N₄O

CAS No.

288150-92-5

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(C)=NC2=C(C=C(C=C21)F)F)NC3=CC=C(C=C3)N(C)C

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 : 50 mg/mL (140.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8061 mL	14.0304 mL	28.0608 mL
5 mM	0.5612 mL	2.8061 mL	5.6122 mL
10 mM	0.2806 mL	1.4030 mL	2.8061 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.27%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (248 KB) HNMR (163 KB) LCMS (418 KB)

Handling Instructions (2659 KB)

References

[1]. Langmead CJ, et al. Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. Br J Pharmacol. 2004;141(2):340-346. [Content Brief]

[2]. Kis GK, et al. The osmotically and histamine-induced enhancement of the plasma vasopressin level is diminished by intracerebroventricularly administered orexin in rats. Pflugers Arch. 2012;463(4):531-536. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8061 mL	14.0304 mL	28.0608 mL	70.1520 mL
	5 mM	0.5612 mL	2.8061 mL	5.6122 mL	14.0304 mL
	10 mM	0.2806 mL	1.4030 mL	2.8061 mL	7.0152 mL
	15 mM	0.1871 mL	0.9354 mL	1.8707 mL	4.6768 mL
	20 mM	0.1403 mL	0.7015 mL	1.4030 mL	3.5076 mL
	25 mM	0.1122 mL	0.5612 mL	1.1224 mL	2.8061 mL
	30 mM	0.0935 mL	0.4677 mL	0.9354 mL	2.3384 mL
	40 mM	0.0702 mL	0.3508 mL	0.7015 mL	1.7538 mL
	50 mM	0.0561 mL	0.2806 mL	0.5612 mL	1.4030 mL
	60 mM	0.0468 mL	0.2338 mL	0.4677 mL	1.1692 mL
	80 mM	0.0351 mL	0.1754 mL	0.3508 mL	0.8769 mL
	100 mM	0.0281 mL	0.1403 mL	0.2806 mL	0.7015 mL

SB-408124 Related Classifications

Neurological Disease Endocrinology

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.

Keywords:

SB-408124288150-92-5SB408124SB 408124Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorcellmembraneselectivitywaterintakeInhibitorinhibitorinhibit

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