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Ketanserin tartrate

Cat. No. M13869
Ketanserin tartrate Structure
Synonym:

R41468 tartrate

Size Price Availability Quantity
50mg USD 55  USD55 In stock
100mg USD 80  USD80 In stock
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Quality Control & Documentation
Biological Activity

Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).

Chemical Information
Molecular Weight 545.51
CAS Number 83846-83-7
Solubility (25°C) DMSO 100 mg/mL
Water 6 mg/mL
Storage 2-8°C, dry, sealed
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] Wen-Jin Xu, et al. Neuroreport. Involvement of 5-HT2A, 5-HT2B and 5-HT2C receptors in mediating the ventrolateral orbital cortex-induced antiallodynia in a rat model of neuropathic pain

[2] Monika Kubacka, et al. Eur J Pharmacol. Anti-aggregation effect of aroxyalkyl derivatives of 2-methoxyphenylpiperazine is due to their 5-HT 2A and α 2-adrenoceptor antagonistic properties. A comparison with ketanserin, sarpogrelate, prazosin, yohimbine and ARC239

[3] H Nakamura, et al. Drugs. Effects of ketanserin tartrate on serum lipids in patients with essential hypertension

[4] M Suzukawa, et al. Eur J Clin Pharmacol. Effect of ketanserin tartrate on HMG CoA reductase and LDL receptor activity in cultured human skin fibroblasts

[5] M Suzukawa, et al. Cardiovasc Drugs Ther. Effects of ketanserin tartrate on 3-hydroxy, 3-methylglutaryl coenzyme A reductase activity in cultured human skin fibroblasts

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