| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
5-HT7 Receptor (pKi = 7.5)
|
|---|---|
| ln Vitro |
Without significantly altering the peak response to 5-CT, SB-258719 (1, 3 and 10 μM; HEK 293 cells) hydrochloride induces a concentration-related rightward shift in the 5-CT concentration response curve [1].
|
| ln Vivo |
SB-258719 hydrochloride (5~20 mg/kg; intraperitoneal injection) can considerably reduce the hypothermia brought on by 5-CT [2].
|
| Enzyme Assay |
Measurement of [35S]-GTPgS binding [ 35S]-GTPgS binding to 5-HT7(a)/HEK293 membranes was measured using the method of Thomas et al. (1995a). Brie¯y, membranes (20 ± 30 mg protein) were preincubated (308C for 30 min) in 20 mM HEPES buer (pH 7.4) in the presence of 3 mM MgCl2, 100 mM NaCl, 10 mM GDP, 0.2 mM ascorbate and in the presence or absence of test drugs. Incubations (30 min, 308C) were started by addition of [ 35S]-GTPgS (0.1 ± 3 nM) followed by vigorous mixing and stopped by rapid ®ltration through Whatman GF/B ®lters followed by ®ve 1 ml washes with ice-cold buer containing 20 mM HEPES and 3 mM MgCl2. All determinations within an experiment were performed in duplicate. Radioactivity on the ®lters was determined using liquid scintillation spectrometry.[1]
|
| Cell Assay |
HEK293 cells stably expressing the human 5-HT7(a) receptor were grown in Minimum Essential Medium (MEM) containing 10% dialysed foetal calf serum, G418 sulphate (1 mM), glutamine (2 mM) and non-essential amino acids (1%). Cells were grown to con¯uence, washed with phosphate buered saline (PBS), and pelleted by centrifugation (1000 g) in PBS containing EDTA (0.1 mM) and dithiothreitol (1 mM). Pellets were stored at 7808C prior to membrane preparation. For preparation of membranes, cell pellets were washed twice by homogenisation (Polytron, 15 s, setting 5) and centrifugation (50,000 g, 15 min, 48C) in 20 volumes of Tris HCl (25 mM pH 7.4) containing EDTA (0.1 mM). Membranes were then resuspended in buer and incubated (378C, 20 min). Following centrifugation and a further wash at 48C, the membranes were ®nally re-suspended at a membrane concentration equivalent to 2.56107 cells ml71 and stored at 7808C prior to use[1].
|
| Animal Protocol |
Animal/Disease Models: Male Swiss Webster mouse (20~25 g) [2].
Doses: 5~20 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results:Dramatically attenuated hypothermia caused by 5-CT. |
| References |
|
| Molecular Formula |
C18H31CLN2O2S
|
|---|---|
| Molecular Weight |
374.97
|
| Exact Mass |
374.179
|
| Elemental Analysis |
C, 57.66; H, 8.33; Cl, 9.45; N, 7.47; O, 8.53; S, 8.55
|
| CAS # |
1217674-10-6
|
| Related CAS # |
SB 258719;195199-95-2
|
| PubChem CID |
56972181
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
24
|
| Complexity |
452
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
Cl.S(C1C=CC=C(C)C=1)(N(C)[C@H](C)CCN1CCC(C)CC1)(=O)=O
|
| InChi Key |
UIZKHTBWJSUGOV-UNTBIKODSA-N
|
| InChi Code |
InChI=1S/C18H30N2O2S.ClH/c1-15-8-11-20(12-9-15)13-10-17(3)19(4)23(21,22)18-7-5-6-16(2)14-18;/h5-7,14-15,17H,8-13H2,1-4H3;1H/t17-;/m1./s1
|
| Chemical Name |
N,3-dimethyl-N-[(2R)-4-(4-methylpiperidin-1-yl)butan-2-yl]benzenesulfonamide Hydrochloride
|
| Synonyms |
SB 258719 HCl; SB258719; SB 258719; SB 258719;SB 258719 hydrochloride; 1217674-10-6; SB-258719 hydrochloride; SB 258719 (hydrochloride); 3-METHYL-N-[(1R)-1-METHYL-3-(4-METHYL-1-PIPERIDINYL)PROPYL]-N-METHYLBENZENESULFONAMIDE HYDROCHLORIDE; N,3-dimethyl-N-[(2R)-4-(4-methylpiperidin-1-yl)butan-2-yl]benzenesulfonamide;hydrochloride; 3-Methyl-N-[(1R)-1-methyl-3-(4-methyl-1-piperidinyl)propyl]-N-methylbenzenesulfonamidehydrochloride; SB258719 hydrochloride;
|
| 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 (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6669 mL | 13.3344 mL | 26.6688 mL | |
| 5 mM | 0.5334 mL | 2.6669 mL | 5.3338 mL | |
| 10 mM | 0.2667 mL | 1.3334 mL | 2.6669 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.
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.
(2) Be sure to add the solvent(s) in order.
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