RS 127445

5-HT2B receptor antagonist,high affinity CAS# 199864-87-4

RS 127445

Catalog No. BCC1909----Order now to get a substantial discount!

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Chemical structure

RS 127445

3D structure

Chemical Properties of RS 127445

Cas No. 199864-87-4 SDF Download SDF
PubChem ID 196968 Appearance Powder
Formula C17H17ClFN3 M.Wt 317.79
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name 4-(4-fluoronaphthalen-1-yl)-6-propan-2-ylpyrimidin-2-amine
SMILES CC(C)C1=NC(=NC(=C1)C2=CC=C(C3=CC=CC=C32)F)N
Standard InChIKey ZZZQXCUPAJFVBN-UHFFFAOYSA-N
Standard InChI InChI=1S/C17H16FN3/c1-10(2)15-9-16(21-17(19)20-15)13-7-8-14(18)12-6-4-3-5-11(12)13/h3-10H,1-2H3,(H2,19,20,21)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of RS 127445

DescriptionRS 127445 is a high affinity antagonist of 5-HT2B receptor with pKi value of 9.5.
Targets5-HT2B receptor    
IC509.5 (pKi)     

RS 127445 Dilution Calculator

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RS 127445 Molarity Calculator

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Preparing Stock Solutions of RS 127445

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1467 mL 15.7337 mL 31.4673 mL 62.9346 mL 78.6683 mL
5 mM 0.6293 mL 3.1467 mL 6.2935 mL 12.5869 mL 15.7337 mL
10 mM 0.3147 mL 1.5734 mL 3.1467 mL 6.2935 mL 7.8668 mL
50 mM 0.0629 mL 0.3147 mL 0.6293 mL 1.2587 mL 1.5734 mL
100 mM 0.0315 mL 0.1573 mL 0.3147 mL 0.6293 mL 0.7867 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on RS 127445

RS-127445(MT 500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4 [1].

5-HT2B receptor belongs to the 5-HT2 receptor family which binds the neurotransmitter serotonin. It plays important role relevant to serotonin, including neuronal sensitization to tactile stimuli.

RS 127445 is a selective serotonin 5-HT2B receptor inhibitor. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor [2]. RS-127445 potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine.

In rat model, oral administration of RS-127445 at 1 to 10 mg/kg resulted in significant inhibition of visceral hypersensitivity up to 35 to 74% triggered by restraint stress [3]. Moreover, 3 to 30 mg/ kg of RS-127445 resulted in a significant inhibition of TNBS-induced visceral hypersensitivity varied from 15 to 62% [3].

References:
[1].  O'Mahony, S M et al. 5-HT2B receptors modulate visceral hypersensitivity in a stress-sensitive animal model of brain-gut axis dysfunction. Neurogastroenterology & Motility, 2012, 22(5): 573-578.
[2].  Ohashi-Doi K et al. A selective, high affinity 5-HT2B receptor antagonist inhibits visceral hypersensitivity in rats. Neurogastroenterology & Motility, 2010, 22(2): 69-76.
[3].  Bassil A K et al. Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology. British Journal of Pharmacology, 2009, 158(1): 252-258.

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References on RS 127445

Inhibition of colonic motility and defecation by RS-127445 suggests an involvement of the 5-HT2B receptor in rodent large bowel physiology.[Pubmed:19371340]

Br J Pharmacol. 2009 Sep;158(1):252-8.

BACKGROUND: 5-HT(2B) receptors are localized within the myenteric nervous system, but their functions on motor/sensory neurons are unclear. To explore the role of these receptors, we further characterized the 5-HT(2B) receptor antagonist RS-127445 and studied its effects on peristalsis and defecation. EXPERIMENTAL APPROACH: Although reported as a selective 5-HT(2B) receptor antagonist, any interactions of RS-127445 with 5-HT(4) receptors are unknown; this was examined using the recombinant receptor and Biomolecular Interaction Detection technology. Mouse isolated colon was mounted in tissue baths for isometric recording of neuronal contractions evoked by electrical field stimulation (EFS), or under an intraluminal pressure gradient to induce peristalsis; the effects of RS-127445 on EFS-induced and on peristaltic contractions were measured. Faecal output of rats in grid-bottom cages was measured over 3 h following i.p. RS-127445 and separately, validation of the effective doses was achieved by determining the free, unbound fraction of RS-127445 in blood and brain. KEY RESULTS: RS-127445 (up to 1 micromol x L(-1)) did not interact with the 5-HT(4) receptor. RS-127445 (0.001-1 micromol x L(-1)) did not affect EFS-induced contractions of the colon, although at 10 micromol x L(-1) the contractions were reduced (to 36 +/- 8% of control, n= 4). RS-127445 (0.1-10 micromol x L(-1)) concentration-dependently reduced peristaltic frequency (n= 4). RS-127445 (1-30 mg x kg(-1)), dose-dependently reduced faecal output, reaching significance at 10 and 30 mg x kg(-1) (n= 6-11). In blood and brain, >98% of RS-127445 was protein-bound. CONCLUSIONS AND IMPLICATIONS: High-protein binding of RS-127445 indicates that relatively high doses are required for efficacy. The results suggest that 5-HT(2B) receptors tonically regulate colonic motility.

RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist.[Pubmed:10455251]

Br J Pharmacol. 1999 Jul;127(5):1075-82.

Efforts to define precisely the role of 5-HT2B receptors in normal and disease processes have been hindered by the absence of selective antagonists. To address this deficiency, we developed a series of naphthylpyrimidines as potentially useful 5-HT2B receptor antagonists. RS-127445 (2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine) was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3). RS-127445 had no detectable intrinsic activity in these assays. In rats, the fraction of RS-127445 that was bioavailable via the oral or intraperitoneal routes was 14 and 60% respectively. Intraperitoneal administration of RS-127445 (5 mg kg(-1)) produced plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4 h. In conclusion, RS-127445 is a selective, high affinity 5-HT2B receptor antagonist suitable for use is vivo. The therapeutic potential of this molecule is being further evaluated.

Description

RS-127445 is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors.

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