SB 216641 hydrochloride

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Cat.No. 1242 - SB 216641 hydrochloride | C28H30N4O4.HCl | CAS No. 193611-67-5
Description: Selective h5-HT1B antagonist
Chemical Name: N-[3-[3-(Dimethylamino)ethoxy]-4-methoxyphenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (5)
Reviews (1)
Literature (4)

Biological Activity

A selective h5-HT1B antagonist with approximately 25-fold selectivity over h5-HT1D and little or no affinity for a range of other receptor types.

Licensing Information

Sold with the permission of GlaxoSmithKline

Technical Data

M. Wt 523.03
Formula C28H30N4O4.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 193611-67-5
PubChem ID 10392025
InChI Key JPBMDMNORXKGHZ-UHFFFAOYSA-N
Smiles Cl.COC1=C(OCCN(C)C)C=C(NC(=O)C2=CC=C(C=C2)C2=CC=C(C=C2C)C2=NOC(C)=N2)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 26.15 50

Preparing Stock Solutions

The following data is based on the product molecular weight 523.03. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 3.82 mL 19.12 mL 38.24 mL
2.5 mM 0.76 mL 3.82 mL 7.65 mL
5 mM 0.38 mL 1.91 mL 3.82 mL
25 mM 0.08 mL 0.38 mL 0.76 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Hagan et al (1997) Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig. Eur.J.Pharmacol. 331 169 PMID: 9274976

Price et al (1997) SB-216641 and BRL-15572 - compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. Naunyn Schmiedebergs Arch.Pharmacol. 356 312 PMID: 930567

Schlicker et al (1997) Effects of selective h5-HT1B (SB-216641) and 5-HT1D (BRL-15572) receptor ligands on guinea pig and human 5-HT auto- and heteroreceptors. Naunyn Schmiedebergs Arch.Pharmacol. 356 321 PMID: 9303568


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Keywords: SB 216641 hydrochloride, SB 216641 hydrochloride supplier, Selective, h5-HT1B, antagonist, Serotonin, Receptors, SB216641, hydrochloride, GlaxoSmithKline, GSK, 5-HT1B, 1242, Tocris Bioscience

5 Citations for SB 216641 hydrochloride

Citations are publications that use Tocris products. Selected citations for SB 216641 hydrochloride include:

Krishnan (2016) Amygdala-hippocampal phospholipase D (PLD) signaling as novel mechanism of cocaine-environment maladaptive conditioned responses. Int.J.Neuropsychopharmacol. 19 1 PMID: 26802567

Soll et al (2012) Expression of serotonin receptors in human hepatocellular cancer. Clin Cancer Res 18 5902 PMID: 23087410

Dunbar et al (2010) Endogenous extracellular serotonin modulates the spinal locomotor network of the neonatal mouse. J Physiol 588 139 PMID: 19884315

Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728


Do you know of a great paper that uses SB 216641 hydrochloride from Tocris? Please let us know.

Reviews for SB 216641 hydrochloride

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Excellent product.
By Anonymous on 06/03/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: CHO

1µM

After reaching 80% confluence, cells were treated with the selective 5-HT2CR antagonist SB242084 (300nM) or the 5-HT1BR antagonist SB216641 (1µM), applied 10 minutes prior to agonist application.

PMID: 26802567 Reference
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