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SB742457 (Intepirdine)

Cat. No. M3000
SB742457 (Intepirdine) Structure
Synonym:

GSK 742457; Intepirdine

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 50  USD50 In stock
5mg USD 100  USD100 In stock
10mg USD 160  USD160 In stock
25mg USD 340  USD340 In stock
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Quality Control & Documentation
Biological Activity

SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors.

Customer Product Validations & Biological Datas
Source Psychopharmacology (2016). Figure 2. SB742457
Method i.v.
Cell Lines mice
Concentrations 3.0 mg/kg
Incubation Time 30 and 60 min
Results In comparison to the vehicle response, there was a significant reduction in glucose solution consumed after the 3.0 mg/kg dose of SB-742457
Chemical Information
Molecular Weight 353.44
Formula C19H19N3O2S
CAS Number 607742-69-8
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gareth Maher-Edwards, et al. Two randomized controlled trials of SB742457 in mild-to-moderate Alzheimer's disease

[2] Christine A Parker, et al. Human Kinetic Modeling of the 5HT6 PET Radioligand 11C-GSK215083 and Its Utility for Determining Occupancy at Both 5HT6 and 5HT2A Receptors by SB742457 as a Potential Therapeutic Mechanism of Action in Alzheimer Disease

[3] Charlotte K Callaghan, et al. Age-related declines in delayed non-match-to-sample performance (DNMS) are reversed by the novel 5HT6 receptor antagonist SB742457

[4] Xabier Codony, et al. 5-HT(6) receptor and cognition

[5] Marieke Liem-Moolenaar, et al. Central nervous system effects of the interaction between risperidone (single dose) and the 5-HT6 antagonist SB742457 (repeated doses) in healthy men

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Keywords: SB742457 (Intepirdine), GSK 742457; Intepirdine supplier, 5-HT Receptor, inhibitors, activators


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