SB-334867

Alias: SB334867A; SB334867; SB 334867; SB334867 HCl; SB334867 hydrochloride; SB-334867A; SB 334867A

Cat No.:V2577 Purity: = 100%

COA Product Data Instructions for use SDS

SB-334867 is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with a pKb value of 7.2.

SB-334867 Chemical Structure CAS No.: 792173-99-0
Product category: OX Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of SB-334867:

SB-334867 HCl

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

InvivoChem's SB-334867 has been cited by 1 publication

[1] Behav Brain Res. 2023 Feb 13:438:114171.

Purity & Quality Control Documentation

Current batch：

Purity: = 100%

COA

MSDS

NMR

HPLC

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

SB-334867 is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with a pKb value of 7.2. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been demonstrated to have sedative and anorectic effects in animals. It has also proven helpful in defining how orexinergic regulation of brain systems related to appetite, sleep, and other physiological processes is regulated.

Biological Activity I Assay Protocols (From Reference)

Targets

OX1 receptor

ln Vitro

In vitro activity: SB-334867 inhibits the calcium responses induced by orexin-A (10 nM) and orexin-B (100 nM) in a concentration-dependent manner, with apparent pKb values of 7.27±0.04 and 7.23±0.03. However, it has no effect on the calcium response elicited by UTP (3 μM), which activates an endogenous purinergic receptor in CHO-OX1 and CHO-OX2 cells[4].

ln Vivo

SB-334867 (20 mg/kg intraperitoneal injection; 20 days) when compared to the occasionally morphine-treated group, can dramatically reduce the effect of the morphine challenge dose in mice when given 15 minutes prior to morphine injection[2].
SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) dramatically lowers ethanol intake in comparison to the vehicle while having no effect on water consumption in female P rats[3].
SB334867 (intraperitoneal injection; 3, 10 and 30 mg/kg) decreases the amount of ethanol consumed at the 30 mg/kg dose, suppresses the amount of sucrose consumed in relation to the vehicle, and lowers blood ethanol concentrations (BECs) in comparison to the 10 and 30 mg/kg doses[3].

Enzyme Assay

SB-334867 free base has an IC50 value of 7.2 (pKb) and is a selective non-peptide orexin OX1 receptor antagonist. In CHO-OX(1) cells, SB-334867-A did not affect the calcium response induced by UTP (3 microM) but it did suppress the responses to orexin-A (10 nM) and orexin-B (100 nM) (pK(B)=7.27+/-0.04 and 7.23+/-0.03, respectively, n=8). The calcium responses mediated by OX(2) were also inhibited by SB-334867-A (10 microM) (32.7+/-1.9% versus orexin-A).

Cell Assay

Two peptides extracted from the rat hypothalamus are called orexin-A and orexin-B. Some physiological processes that they are involved in include feeding regulation, energy metabolism, and sleep-wake cycle regulation. In CHO-OX1 cells, SB-334867 can suppress the calcium responses induced by orexin-A and orexin-B, with pKB values of 7.27 and 7.23, respectively. For OX1 receptors, SB-334867 exhibits greater selectivity than OX2 receptors. It inhibits the calcium responses in CHO-OX2 cells that are induced by orexin-A by 32.7% and orexin-B by 22%, respectively.

Animal Protocol

Dissolved in 10% (w/v) Encapsin in sterile water; 30 mg/kg; i.p. administration

Male and female Sprague–Dawley rats

References

[1]. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.Bioorg Med Chem Lett. 2001 Jul 23;11(14):1907-10.

[2]. SB-334867 (an Orexin-1 Receptor Antagonist) Effects on Morphine-Induced Sensitization in Mice-a View on Receptor Mechanisms.

[3]. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models.Front Neurosci. 2014 Feb 25;8:33.

[4]. SB-334867-A: the first selective orexin-1 receptor antagonist.Br J Pharmacol. 2001 Mar;132(6):1179-82.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C17H13N5O2

Molecular Weight

319.32

Exact Mass

319.11

Elemental Analysis

C, 63.94; H, 4.10; N, 21.93; O, 10.02

CAS #

792173-99-0

Related CAS #

SB-334867; 249889-64-3

Appearance

Solid powder

SMILES

CC1=NC2=C(O1)C=C(C=C2)NC(=O)NC3=C4C(=NC=C3)C=CC=N4

InChi Key

AKMNUCBQGHFICM-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H13N5O2/c1-10-20-12-5-4-11(9-15(12)24-10)21-17(23)22-14-6-8-18-13-3-2-7-19-16(13)14/h2-9H,1H3,(H2,18,21,22,23)

Chemical Name

1-(2-methyl-1,3-benzoxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea

Synonyms

SB334867A; SB334867; SB 334867; SB334867 HCl; SB334867 hydrochloride; SB-334867A; SB 334867A

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: ~63 mg/mL (~197.3 mM)

Water: <1 mg/mL

Ethanol:~3 mg/mL (~9.4 mM)

Solubility (In Vivo)

1%CMC Na: 30mg/mL

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.1317 mL	15.6583 mL	31.3165 mL
	5 mM	0.6263 mL	3.1317 mL	6.2633 mL
	10 mM	0.3132 mL	1.5658 mL	3.1317 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

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Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Biological Data

SB-334867-A inhibits human OX1 receptor-mediated calcium responses in a concentration-dependent manner.Br J Pharmacol. 2001 Mar; 132(6): 1179–1182.

SB-334867 HCl — Effects of olanzapine (3 mg/kg, i.v.) followed 30 min later by administration of the SB-334867 (SB; 2 mg/kg, i.v.) or vehicle (veh) on the firing rate of locus coeruleus (LC) neurons.Neuropsychopharmacology.2007 Apr;32(4):786-92.