Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
SB271046 HCl (SB 271046; SB-271046), the hydrochloride salt of SB 271046, is a novel, potent, selective and orally bioactive 5-HT6 receptor antagonist with potential anticonvulsant activity. It has 200 times more selectivity than other 5-HT receptor subtypes and inhibits 5-HT6 with a pKi of 8.9.
Targets |
5-HT6 Receptor ( pKi = 8.92-9.02 ); 5-HT1D Receptor ( pKi = 6.55 ); 5-HT1A Receptor ( pKi = 6.35 ); 5-HT1B Receptor ( pKi = 6.05 ); 5-HT1F Receptor ( pKi = 5.95 );
5-HT2A Receptor ( pKi = 5.62 ); 5-HT2B Receptor ( pKi = 5.41 ); 5-HT7 Receptor ( pKi = 5.39 ); 5-HT4 ( pKi = 5.27 ); 5-HT1E ( pKi < 4.99 ); Human 5-HT2C Receptor ( pKi = 5.73 ) |
||
---|---|---|---|
ln Vitro |
|
||
ln Vivo |
|
||
Enzyme Assay |
SB271046 Hcl is an effective, pKi of 8.9, selective, and oral 5-HT6 receptor antagonist. IC50 Value: 8.9(pKi). A sulfonamidal benzothiophene derivative, SB 271046 hydrochloride has been demonstrated to function as a selective 5-HT6 antagonist, with pKi values of 9.02-8.92, 6.55, 6.35, 6.27, 6.05, 5.95, 5.76, 5.73, 5.62, 5.55, 5.41, 5.39, 5.27, and < 4.99 for 5-HT6, 5-HT1D, 5-HT1A, D3, 5-HT1B, 5-HT1F, α1B, 5-HT2C, 5-HT2A, D2, 5-HT2B, 5-HT7, 5-HT4 and 5-HT1E, respectively. It is also > 200-fold selective over 55 other receptors, enzymes, and ion channels.
|
||
Animal Protocol |
|
||
References |
Molecular Formula |
C20H23CL2N3O3S2
|
|
---|---|---|
Molecular Weight |
488.45
|
|
Exact Mass |
487.06
|
|
Elemental Analysis |
C, 49.18; H, 4.75; Cl, 14.52; N, 8.60; O, 9.83; S, 13.13
|
|
CAS # |
209481-24-3
|
|
Appearance |
Solid powder
|
|
SMILES |
CC1=C(SC2=C1C=C(C=C2)Cl)S(=O)(=O)NC3=CC(=C(C=C3)OC)N4CCNCC4.Cl
|
|
InChi Key |
RMXZRJYGJMSDQK-UHFFFAOYSA-N
|
|
InChi Code |
InChI=1S/C20H22ClN3O3S2.ClH/c1-13-16-11-14(21)3-6-19(16)28-20(13)29(25,26)23-15-4-5-18(27-2)17(12-15)24-9-7-22-8-10-24;/h3-6,11-12,22-23H,7-10H2,1-2H3;1H
|
|
Chemical Name |
5-chloro-N-(4-methoxy-3-piperazin-1-ylphenyl)-3-methyl-1-benzothiophene-2-sulfonamide;hydrochloride
|
|
Synonyms |
|
|
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) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0473 mL | 10.2365 mL | 20.4729 mL | |
5 mM | 0.4095 mL | 2.0473 mL | 4.0946 mL | |
10 mM | 0.2047 mL | 1.0236 mL | 2.0473 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.