SB-334867 HCl

Alias: SB334867A; SB334867; SB 334867; SB334867 HCl; SB334867 hydrochloride; SB-334867A; SB 334867A
Cat No.:V1309 Purity: ≥98%
SB-334867 HCl (SB-334867A; SB334867; SB 334867),the hydrochloride salt ofSB-334867, is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with the potential for treating sleeping disorders.
SB-334867 HCl Chemical Structure CAS No.: 249889-64-3
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 HCl:

  • SB-334867
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's SB-334867 HCl has been cited by 1 publication
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SB-334867 HCl (SB-334867A; SB334867; SB 334867), the hydrochloride salt of SB-334867, is a novel, non-peptide, selective orexin-1 (OX1) receptor antagonist with the potential for treating sleeping disorders. It inhibits orexin-1 with a pKb value of 7.2. It was the first non-peptide antagonist to be developed with selectivity 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)
ln Vitro

In vitro activity: SB-334867 has no effect on the UTP (3 microM)-induced calcium response, but it inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses in CHO-OX1 cells, with pKB values of 7.27 and 7.23, respectively.

ln Vivo
SB-334867 (30 mg/kg, i.p.) dramatically lowers food intake in both naturally occurring and orexin-A-induced rats, both male and female. In rats, the effects of antipsychotic medications on dopamine neuronal activity are blocked by SB-334867 (2 mg/kg, i.v.). Additionally, SB-334867 prevents rats from developing a tolerance to morphine analgesics.
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]. Br J Pharmacol . 2001 Mar;132(6):1179-82.

[2]. Neuropsychopharmacology . 2007 Apr;32(4):786-92.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H14NCLN5O2
Molecular Weight
319.32
Exact Mass
319.11
Elemental Analysis
C, 57.39; H, 3.97; Cl, 9.96; N, 19.68; O, 8.99
CAS #
249889-64-3
Appearance
White to off-white solid powder
SMILES
O=C(NC1=CC=NC2=CC=CN=C12)NC3=CC=C4N=C(C)OC4=C3.[H]Cl
InChi Key
AKMNUCBQGHFICM-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H13N5O2.ClH/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);1H
Chemical Name
1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea hydrochloride
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: 30 mg/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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.

(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.
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Biological Data

  • SB-334867 HCl

    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.


  • SB-334867 HCl
    Effect of chronic administration of olanzapine (OLZ; 10 mg/kg/day, s.c. times 21 days) or vehicle (VEH) and acute administration of SB-334867 (SB; 2 mg/kg, i.v.) on the number of A9 and A10 dopamine cells per track.Neuropsychopharmacology.2007 Apr;32(4):786-92.
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