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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
SB269970 (SB-269970A) is a novel and potent 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors. SB269970 functions as a 5-HT7 receptor selective antagonist that exhibits at least a 100-fold selectivity against 5-HT7 across a range of receptors and enzymes. Moreover, SB269970 suppresses the 5-CT-stimulated adenylyl cyclase activity in both the guinea-pig hippocampal (pKB of 8.3) and 5-HT7(a)/HEK293 (pA2 of 8.5) membranes.
Targets |
5-HT7 Receptor ( pKi = 8.3 )
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
SB269970 an antagonist of the 5-HT7 receptor with pKi of 8.3, exhibits >50-fold selectivity against other receptors. The novel 5-HT(7) receptor antagonist, SB-269970-A, potently displaced [(3)H]-5-CT from human 5-HT(7(a)) (pK(i) 8.9+/-0.1) and 5-HT(7) receptors in guinea-pig cortex (pK(i) 8.3+/-0.2). 5-CT stimulated adenylyl cyclase activity in 5-HT(7(a))/HEK293 membranes (pEC(50) 7.5+/-0.1) and SB-269970-A (0.03 - 1 microM) inhibited the 5-CT concentration-response with no significant alteration in the maximal response. The pA(2) (8.5+/-0.2) for SB-269970-A agreed well with the pK(i) determined from [(3)H]-5-CT binding studies. 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC(50) of 8.4+/-0.2) was inhibited by SB-269970-A (0.3 microM) with a pK(B) (8.3+/-0.1) in good agreement with its antagonist potency at the human cloned 5-HT(7(a)) receptor and its binding affinity at guinea-pig cortical membranes. 5-HT(7) receptor mRNA was highly expressed in human hypothalamus, amygdala, thalamus, hippocampus and testis. SB-269970-A was CNS penetrant (steady-state brain : blood ratio of ca. 0.83 : 1 in rats) but was rapidly cleared from the blood (CLb=ca. 140 ml min(-1) kg(-1))[1].
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Animal Protocol |
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References |
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Additional Infomation |
SB-269970 is an experimental drug developed by GlaxoSmithKline. In the studies performed with this agent, it has been suggested that SB-269970 acts either as a selective antagonist or inverse agonist of the serotonin receptor 7 (5-HT7).
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Molecular Formula |
C18H28N2O3S
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Molecular Weight |
352.49
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Exact Mass |
352.18
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Elemental Analysis |
C, 61.33; H, 8.01; N, 7.95; O, 13.62; S, 9.10
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CAS # |
201038-74-6
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Related CAS # |
SB-269970 hydrochloride; 261901-57-9
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PubChem CID |
6604889
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Appearance |
Solid powder
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Boiling Point |
512.9ºC at 760 mmHg
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Flash Point |
264ºC
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Vapour Pressure |
3.87E-11mmHg at 25°C
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LogP |
4.43
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tPSA |
69.230
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SMILES |
CC1CCN(CC1)CC[C@H]2CCCN2S(=O)(=O)C3=CC=CC(=C3)O
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InChi Key |
HWKROQUZSKPIKQ-MRXNPFEDSA-N
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InChi Code |
InChI=1S/C18H28N2O3S/c1-15-7-11-19(12-8-15)13-9-16-4-3-10-20(16)24(22,23)18-6-2-5-17(21)14-18/h2,5-6,14-16,21H,3-4,7-13H2,1H3/t16-/m1/s1
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Chemical Name |
3-[(2R)-2-[2-(4-methylpiperidin-1-yl)ethyl]pyrrolidin-1-yl]sulfonylphenol
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
30%propylene glycol+ 5%Tween 80+ 65%D5W: 30.0mg/ml (77.13mM) (Please use freshly prepared in vivo formulations for optimal results.)
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8370 mL | 14.1848 mL | 28.3696 mL | |
5 mM | 0.5674 mL | 2.8370 mL | 5.6739 mL | |
10 mM | 0.2837 mL | 1.4185 mL | 2.8370 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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