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RS-127445 hydrochloride

Catalog No. T7519 CAS 199864-86-3

Synonyms: RS 127445, MT 500

RS-127445 hydrochloride (MT 500) is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist(pKi : 9.5).

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RS-127445 hydrochloride Chemical Structure

RS-127445 hydrochloride, CAS 199864-86-3

Pack Size	Availability	Price/USD
5 mg	In stock	$ 47.00
10 mg	In stock	$ 77.00
25 mg	In stock	$ 146.00
50 mg	In stock	$ 262.00
100 mg	In stock	$ 395.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

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Purity: 98%

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Description	RS-127445 hydrochloride (MT 500) is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist(pKi : 9.5).
Targets&IC50	5-HT2B:9.5(pKi)
In vitro	RS 127445 potently displaced [3H]-5-HT from human recombinant 5-HT2B receptors expressed in CHO-K1 cells.?The affinity (pKi value) of RS-127445 for the 5-HT2B receptor was 9.5±0.1 (n=9).?RS-127445 was selective for the 5-HT2B receptor, having approximately 1000 fold lower affinity for the human?recombinant 5-HT2A, 5-HT2C, 5-HT5, 5-HT6 and 5-HT7 receptors, a 5-HT1A receptor in rat brain membranes, a 5-HT1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets[1]
In vivo	RS 127445 (5 mg kg^?1) was administered to rats by oral, intraperitoneal and intravenous routes.?Peak plasma concentrations were rapidly achieved with the highest concentrations being found at the first time-point measured following intravenous and intraperitonael administration (0.08 h) and by 0.25 h following dosing by the oral route of administration.?RS-127445 was cleared from plasma with an estimated terminal elimination half-life of approximately 1.7 h. The bioavailability of RS-127445, when administered by the oral and intraperitoneal routes was approximately 14 and 62% of that obtained by intravenous administration .?To test?whether plasma levels were proportional to the dose administered, RS-127445 was given by the intraperitoneal route at doses of 1, 3 and 10 mg kg^?1.?Increasing the dose of RS-127445 resulted in proportional increases in its concentration in the plasma[1]
Animal Research	Rats were euthanized.?Right and left external jugular veins were dissected, cleaned of connective tissues and cut into ring segments approximately 5 mm long.?Tungsten hooks (0.125 mm diameter) were inserted through the lumen of the vein and connected to tension transducers.?Tissues were kept in 10 ml organ baths containing Kreb's solution supplemented with cocaine (30 μm), corticosterone (30 μm), ketanserin (0.3 μm) and indomethacin (3 μm) at 37°C at a resting tension of 0.5 g.?Prior to the initiation of any studies, monamine oxidases were inactivated by a 30 min pre exposure of the tissue to pargyline (0.1 mm).?The veins were then exposed to 0.1 μm U46619 (9,11-dideoxy-9 α, 11 aα-methano-epoxy-PGF2α;?a thromboxane A2 mimetic) until a stable contraction was attained.?Acetylcholine (0.1 μm) was used to verify the integrity of the endothelium and to determine the maximum amount of nitric?oxide-dependent relaxation that was achievable.?After washout of the acetylcholine and recontraction with U46619, cumulative concentration-response curves to (±)-α-methyl-5-HT were constructed.?When maximum relaxation was reached, the baths were rinsed, and the tissues were maintained undisturbed for 2 h. Antagonists (RS 127445)were then added to the bath and allowed to equilibrate with the tissue for at least 1 h before a second concentration-response curve to (±)-α-methyl-5-HT was generated[1].

Synonyms	RS 127445, MT 500
Molecular Weight	317.79
Formula	C17H17ClFN3
CAS No.	199864-86-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31 mg/mL (97.55 mM)

References and Literature

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]. 1999, 127(5):1075-1082. 2. Devroye, Céline, Haddjeri N , Cathala A , et al. Opposite control of mesocortical and mesoaccumbal dopamine pathways by serotonin 2B, receptor blockade: Involvement of medial prefrontal cortex serotonin 1A, receptors[J]. Neuropharmacology, 2017, 119:91-99.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Inhibitor Library Membrane Protein-targeted Compound Library Anti-Alzheimer's Disease Compound Library Bioactive Compound Library Angiogenesis related Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library Neurotransmitter Receptor Compound Library

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Keywords

RS-127445 hydrochloride 199864-86-3 GPCR/G Protein Neuroscience 5-HT Receptor Inhibitor RS127445 Hydrochloride inhibit RS127445 RS-127445 RS127445 hydrochloride MT500 Serotonin Receptor RS-127445 Hydrochloride RS 127445 MT 500 RS 127445 hydrochloride RS 127445 Hydrochloride MT-500 5-hydroxytryptamine Receptor inhibitor

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