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RS 127445 HCl

Catalog No.
B7848
5-HT2B receptor antagonist,high affinity
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$55.00
In stock
5mg
$50.00
In stock
10mg
$80.00
In stock
50mg
$320.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

RS-127445 is a selective, high affinity 5-HT2B receptor antagonist.

The 5-HT2B receptor is a G-protein coupled receptor. 5-HT2B receptors are widely expressed in peripheral tissues of various species. 5-HT2B receptor expresses throughout the gastrointestinal tract including smooth muscle of the stomach fundus, oesophagus, colon and small intestine. The receptor has also been found in the placenta, uterus, lung and prostate. 5-HT2B receptors are present in many vascular beds and have been localized to both vascular smooth muscle and vascular endothelial cells [1].

RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine) showed nanomolar affinity for the 5-HT2B receptor with the pKi of 9.5 ± 0.1. In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pKB = 9.5 ± 0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4 ± 0.1). RS-127445 blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5 ± 1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9 ± 0.3). In rats, RS-127445 was bioavailable via the oral or intraperitoneal routes.

Reference:
[1] Bonhaus D W, Flippin L A, Greenhouse R J, et al.  RS‐127445: a selective, high affinity, orally bioavailable 5‐HT2B receptor antagonist[J]. British journal of pharmacology, 1999, 127(5): 1075-1082.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt317.79
Cas No.199864-87-4
FormulaC17H17ClFN3
SynonymsRS-127445; MT 500; RS127445
Solubility≥31.8 mg/mL in DMSO; insoluble in H2O; ≥33.15 mg/mL in EtOH
Chemical Name4-(4-fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine hydrochloride
SDFDownload SDF
Canonical SMILESFC1=CC=C(C2=CC(C(C)C)=NC(N)=N2)C3=CC=CC=C31.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description RS 127445 is a high affinity antagonist of 5-HT2B receptor with pKi value of 9.5.
Targets 5-HT2B receptor          
IC50 9.5 (pKi)          

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