SB 216641 hydrochlorideSelective h5-HT1B antagonist CAS# 193611-67-5 |
- SB202190 (FHPI)
Catalog No.:BCC1093
CAS No.:152121-30-7
- BIRB 796 (Doramapimod)
Catalog No.:BCC2535
CAS No.:285983-48-4
- TAK-715
Catalog No.:BCC3968
CAS No.:303162-79-0
- PH-797804
Catalog No.:BCC3672
CAS No.:586379-66-0
- LY2228820
Catalog No.:BCC2528
CAS No.:862507-23-1
- SB 203580 hydrochloride
Catalog No.:BCC4293
CAS No.:869185-85-3
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 193611-67-5 | SDF | Download SDF |
PubChem ID | 10392025 | Appearance | Powder |
Formula | C28H31ClN4O4 | M.Wt | 523.03 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Solubility | Soluble to 50 mM in water | ||
Chemical Name | N-[3-[2-(dimethylamino)ethoxy]-4-methoxyphenyl]-4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]benzamide;hydrochloride | ||
SMILES | CC1=C(C=CC(=C1)C2=NOC(=N2)C)C3=CC=C(C=C3)C(=O)NC4=CC(=C(C=C4)OC)OCCN(C)C.Cl | ||
Standard InChIKey | JPBMDMNORXKGHZ-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C28H30N4O4.ClH/c1-18-16-22(27-29-19(2)36-31-27)10-12-24(18)20-6-8-21(9-7-20)28(33)30-23-11-13-25(34-5)26(17-23)35-15-14-32(3)4;/h6-13,16-17H,14-15H2,1-5H3,(H,30,33);1H | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | 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. |
SB 216641 hydrochloride Dilution Calculator
SB 216641 hydrochloride Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 1.9119 mL | 9.5597 mL | 19.1194 mL | 38.2387 mL | 47.7984 mL |
5 mM | 0.3824 mL | 1.9119 mL | 3.8239 mL | 7.6477 mL | 9.5597 mL |
10 mM | 0.1912 mL | 0.956 mL | 1.9119 mL | 3.8239 mL | 4.7798 mL |
50 mM | 0.0382 mL | 0.1912 mL | 0.3824 mL | 0.7648 mL | 0.956 mL |
100 mM | 0.0191 mL | 0.0956 mL | 0.1912 mL | 0.3824 mL | 0.478 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
- Terrestrosin K
Catalog No.:BCN2935
CAS No.:193605-07-1
- GB 1b
Catalog No.:BCN7385
CAS No.:19360-72-6
- Calcifediol
Catalog No.:BCC4949
CAS No.:19356-17-3
- SB 239063
Catalog No.:BCC1923
CAS No.:193551-21-2
- IPAG
Catalog No.:BCC5662
CAS No.:193527-91-2
- Mulberroside F
Catalog No.:BCN2908
CAS No.:193483-95-3
- Fmoc-Glu(Edans)-OH
Catalog No.:BCC3491
CAS No.:193475-66-0
- Zeylenone
Catalog No.:BCC8268
CAS No.:193410-84-3
- Tartrazine
Catalog No.:BCN2217
CAS No.:1934-21-0
- Co 101244 hydrochloride
Catalog No.:BCC7369
CAS No.:193356-17-1
- 5-Aminoindazole
Catalog No.:BCC8734
CAS No.:19335-11-6
- Lonafarnib
Catalog No.:BCC2331
CAS No.:193275-84-2
- BRL-15572
Catalog No.:BCC5065
CAS No.:193611-72-2
- TAS 301
Catalog No.:BCC6214
CAS No.:193620-69-8
- Methyl 4-hydroxycinnamate
Catalog No.:BCN4014
CAS No.:19367-38-5
- 8beta-Methoxyatractylenolide I
Catalog No.:BCN7594
CAS No.:193694-24-5
- Aminoguanidine hydrochloride
Catalog No.:BCC6795
CAS No.:1937-19-5
- SB 242235
Catalog No.:BCC4171
CAS No.:193746-75-7
- Cortistatin 14
Catalog No.:BCC6010
CAS No.:193829-96-8
- Tinidazole
Catalog No.:BCC4866
CAS No.:19387-91-8
- Fmoc-β-Homo-Leu-OH
Catalog No.:BCC2631
CAS No.:193887-44-4
- 3-Phenyl-1,2-dihydroacenaphthylene-1,2-diol
Catalog No.:BCN7178
CAS No.:193892-33-0
- SC 19220
Catalog No.:BCC6968
CAS No.:19395-87-0
- Fmoc-ß-HoAla-OH
Catalog No.:BCC3225
CAS No.:193954-26-6
Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig.[Pubmed:9274976]
Eur J Pharmacol. 1997 Jul 23;331(2-3):169-74.
The selective, brain penetrant, 5-HT(1B/D) (formerly 5-HT(1D beta/alpha)) receptor agonist SKF-99101H (3-(2-dimethylaminoethyl)-4-chloro-5-propoxyindole hemifumarate) (30 mg/kg i.p.) causes a dose related fall in rectal temperature in guinea pigs which previous studies have shown to be blocked by the non-selective 5-HT(1B/D) receptor antagonist GR-127935 (N-[4-methoxy-3-(4-methyl-1-piperazinyl) phenyl]-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl) [1,1'biphenyl]-4-carboxamide oxalate). The present study shows that the hypothermic response to SKF-99101H is dose-dependently blocked by SB-224289G (1'-methyl-5-(2'-methyl-4'-[(5-methyl-1,2,4-oxadiazol-3-yl)bipheny l-4-yl]carbonyl)-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-pi peridone] hemioxalate) (0.3-10.0 mg/kg p.o.) (ED50 3.62 mg/kg), which is the first compound to be described which is more than 60 fold selective for the 5-HT1B receptor over the 5-HT1D receptor. SB-216641A (N-[3-(2-dimethylamino) ethoxy-4-methoxy-phenyl] 2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-(1,1'-biphenyl)-4-car boxamide hydrochloride) (0.6-20.0 mg/kg i.p.), which is somewhat less selective (30 fold) for the 5-HT1B receptor over the 5-HT1D receptor had a similar effect (ED50 4.43 mg/kg). The brain penetrant 5-HT1D selective receptor antagonist, BRL-15572 (4-(3-chlorophenyl)-alpha-(diphenylmethyl)-1-piperazineethanol+ ++ dihydrochloride) (0.3-100.0 mg/kg i.p.) was inactive. When administered alone neither BRL-15572 (0.1-10 mg/kg i.p.) nor SB-224289G (2.2-22 mg/kg p.o.) had an effect on body temperature. These data demonstrate that 5-HT1B (formerly 5-HT(1D beta)) and not 5-HT1D (formerly 5-HT(1D alpha)) receptors mediate the hypothermic response to SKF-99101H (30 mg/kg i.p.) in guinea pigs. The compounds described are useful pharmacological tools for distinguishing responses to 5-HT1B and 5-HT1D receptors.
Effects of selective h5-HT1B (SB-216641) and h5-HT1D (BRL-15572) receptor ligands on guinea-pig and human 5-HT auto- and heteroreceptors.[Pubmed:9303568]
Naunyn Schmiedebergs Arch Pharmacol. 1997 Sep;356(3):321-7.
Human cerebral cortical slices and synaptosomes, guinea-pig cerebral cortical slices and human right atrial appendages were used to study the effects of SB-216641, a preferential h5-HT1B receptor ligand, and of BRL-15572, a preferential h5-HT1D receptor ligand, on the presynaptic h5-HT1B and h5-HT1B-like autoreceptors in the human and guinea-pig brain preparations, respectively, and on the presynaptic h5-HT1D heteroreceptors in the human atrium. The brain preparations, preincubated with [3H]serotonin ([3H]5-HT), and the segments of atrial appendages, preincubated with [3H]noradrenaline, were superfused with modified Krebs' solution and tritium overflow was evoked electrically (human and guinea-pig cerebral cortex slices and human atrial appendages) or by high K+ (human cerebral cortex synaptosomes). The electrically evoked tritium overflow from guinea-pig cerebral cortex slices was reduced by the 5-HT receptor agonist 5-carboxamidotryptamine (5-CT). This effect was not modified by BRL-15572 (2 microM; concentration 154 times higher than its Ki at h5-HT1D receptors) but was antagonized by SB-216641 (0.1 microM; concentration 100 times higher than its Ki at h5-HT1B receptors; apparent pA2 8.45). SB-216641 (0.1 microM) by itself facilitated, whereas BRL-15572 (2 microM) did not affect, the evoked overflow. In human cerebral cortex slices SB-216641 (0.1 microM) also facilitated, and BRL-15572 (2 microM) again failed to affect, the electrically evoked tritium overflow. In human cerebral cortical synaptosomes, 5-CT reduced the K+-evoked tritium overflow. This response was unaffected by BRL-15572 (300 nM) but antagonized by SB-216641 (15 nM; drug concentrations 23 and 15 times higher than their Ki at h5-HT1D and h5-HT1B receptors, respectively). Both drugs, given alone, did not modify the K+-evoked tritium overflow. In human atrial appendages, the electrically evoked tritium overflow was inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors) but not by SB-216641 (30 nM; 30 times Ki at h5-HT1B receptors). Both drugs by themselves did not change the electrically evoked tritium overflow. In conclusion, SB-216641 behaves as a preferential antagonist at native human 5-HT1B receptors and BRL-15572 as a preferential antagonist at native human 5-HT1D receptors. These compounds are clearly useful tools for the differentiation between human 5-HT1B and 5-HT1D receptors in functional studies.