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Fig. 1 · Structure
Cat. No.
A11165
CAS No.
199864-87-4
Formula
C17H16FN3
Mol. Weight
281.33

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RS-127445

5-HT2B receptor antagonist

RS-127445 is a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.

In Stock

Publications for RS-127445

1 publication citing this product

  1. Takeshi Takayanagi, .et al. , Fujita Medical Journal, 2015, 1(1), 1-5, 2015
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For laboratory research use only. We do not sell to patients.

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Biological Activity

Target & Activity

Target Activity Value
5-HT2B pIC50 10.4
5-HT2B pKi 9.5

Cellular Effect

Cell Line Activity Value Description Reference
CHO-K1 IC50 0.7 nM Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay [PMID: 19307114]
CHO-K1 IC50 19 nM Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibition of serotonin-induced intracellular Ca2+ flux by aequorin luminescence assay in presence of 4% human serum albumin [PMID: 19307114]

Specifications

Manufacturer Adooq Bioscience
Actions Antagonist
CAS Number 199864-87-4
Applications 5-HT2B receptor antagonist
Formula C17H16FN3
Molecular Weight 281.33
Synonyms MT 500; RS127,445
SMILES
CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 54 mg/mL (191.94 mM)
Water Insoluble
Ethanol 8 mg/mL (28.43 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Publications

1 publication citing this product

  1. Takeshi Takayanagi, .et al. , Fujita Medical Journal, 2015, 1(1), 1-5, 2015

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