ChemicalBook > CAS DataBase List > 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE

Product Name
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
CAS No.
199864-87-4
Chemical Name
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
Synonyms
445;MT500;RS127;RS 127;RS-127;RS127445;RS-127445HCl;RS 127445 hydrochlor;RS 127445 HYDROCHLORIDE;2,7-Naphthyridin-1(8H)-one
CBNumber
CB92456354
Molecular Formula
C17H16FN3
Formula Weight
281.33
MOL File
199864-87-4.mol
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4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Property

Density 
1.213
storage temp. 
Inert atmosphere,2-8°C
solubility 
≥31.8 mg/mL in DMSO; insoluble in H2O; ≥33.15 mg/mL in EtOH
form 
solid
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical
Product number
23451
Product name
RS 127445
Purity
≥98%
Packaging
1mg
Price
$28
Updated
2022/04/27
Cayman Chemical
Product number
23451
Product name
RS 127445
Purity
≥98%
Packaging
5mg
Price
$96
Updated
2022/04/27
Cayman Chemical
Product number
23451
Product name
RS 127445
Purity
≥98%
Packaging
10mg
Price
$177
Updated
2022/04/27
Tocris
Product number
2993
Product name
RS-127445 hydrochloride
Purity
≥98%(HPLC)
Packaging
10
Price
$203
Updated
2021/12/16
Tocris
Product number
2993
Product name
RS-127445 hydrochloride
Purity
≥98%(HPLC)
Packaging
50
Price
$820
Updated
2021/12/16
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4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Chemical Properties,Usage,Production

Description

RS 127445 is an orally bioavailable and potent antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.32 nM). It is selective for 5-HT2B over other 5-HT receptor subtypes (Ki = >3 μM for 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, 5-HT3, 5-HT5, and 5-HT6). RS 127445 reduces contraction of rat isolated stomach fundus (pA2 = 9.5) and lowers intracellular increases in calcium (IC50 = 0.04 nM) induced by 5-HT . It also blocks (±)-α-methyl-5-HT-induced relaxation of isolated rat jugular veins (pA2 = 9.95). RS 127445 (1-30 mg/kg) reduces peristaltic frequency and fecal output in mice in a dose-dependent manner. Systemic administration of RS 127445 (0.16 mg/kg) reduces basal, but not cocaine-induced, dopamine outflow in the nucleus accumbens of rats and decreases hyperlocomotion induced by cocaine (Item Nos. ISO60176 | 16186 | 22165) or quinpirole.

Uses

RS-127445 is a 5-HT2B receptor antagonist with modest activity against other 5-HT receptors. Selective 5-HT2B receptor antagonist

Biological Activity

High affinity 5-HT 2B receptor antagonist (pK i = 9.5). Displays 1000-fold selectivity for 5-HT 2B with good bioavailability.

in vitro

RS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. RS-127445 is thus among the highest affinity, most selective 5- HT2B receptor ligands. 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 vivo

RS-127445 is readily absorbed with no obvious dose or route-dependent limitations and rapidly absorbed following both oral and intraperitoneal administration with peak plasma concentrations being achieved within 15 min of dosing. RS-127445 concentration in the plasma are achieved are proportional to the administered dose. RS-127445 administrated at dose of 5 mg/kg with approximately 60% of an intraperitoneal dose and 14% of the oral dose is bioavailable. RS-127445 concentration in the plasma is predicted to fully saturate accessible 5-HT2B receptors can be readily achieved and maintained in the rat. RS-127445 administered at 1 to 10 mg/kg with oral significantly inhibits visceral hypersensitivity up to 35 to 74% provoked by restraint stress. Oral RS-127445 produces a significant suppression of TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/ kg), although RS-127445 has no significant effect on the visceral nociceptive threshold of native rats. RS-127445 administrated orally with 1 to 30 mg/kg also dose -dependently reduce the restraint stress-induced defecation in native and TNBS-treated rats. . RS-127445 inhibits colonic motility and defecation.

target

5-HT2B receptor

References

[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.

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Preparation Products And Raw materials

Raw materials

Preparation Products

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4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Suppliers

Shanghai Boyle Chemical Co., Ltd.
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86-21-57758967
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China
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3B Pharmachem (Wuhan) International Co.,Ltd.
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821-50328103-801 18930552037
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86-21-50328109
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3bsc@sina.com
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China
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Shanghai civi chemical technology co.,Ltd
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86-21-34053660
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86-21-34053661
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sale@labgogo.com
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China
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NCE Biomedical Co.,Ltd.
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AdooQ BioScience, LLC
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+1 (866) 930-6790
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+1 (866) 333-9607
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United States
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TargetMol Chemicals Inc.
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AdooQ Bioscience CHINA
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LETOPHARM LIMITED
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Shanghaizehan biopharma technology co., Ltd.
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021-61350663 13052117465
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DebyeTec.com Inc.
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View Lastest Price from 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE manufacturers

Career Henan Chemical Co
Product
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE 199864-87-4
Price
US $3.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
200KG
Release date
2020-01-08

199864-87-4, 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDERelated Search:


  • 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
  • RS 127445 HYDROCHLORIDE
  • 4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine
  • MT500
  • RS127445
  • 2-PyriMidinaMine, 4-(4-fluoro-1-naphthalenyl)-6-(1-Methylethyl)-
  • 4-(4-Fluoronaphthalen-1-yl)-6-isopropylpyriMidin-2-aMine hydrochloride
  • RS-127445HCl
  • 4-(4-Fluoronaphthalen-1-yl)-6-isopropylpyrimidin-2-amine
  • 2-Amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine
  • RS 127445 hydrochloride,4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinaminehydrochloride
  • 445
  • RS 127
  • RS127
  • RS-127
  • RS-127445;RS 127445;RS127445;RS127;445;RS 127;445;RS-127;445
  • Ziprasidone4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
  • MT500;MT 500;RS 127445;RS127445;RS127;445;RS 127;445;RS-127;445
  • 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE USP/EP/BP
  • 4-(4-fluoronaphthalen-1-yl)-6-propan-2-ylpyrimidin-2-amine
  • RS 127445 hydrochlor
  • 2,7-Naphthyridin-1(8H)-one
  • 199864-87-4
  • 199864-87-3
  • C17H17ClFN3
  • C17H16FN3HCl
  • Inhibitors