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;RS-127445, 10 mM in DMSO
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
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H301Toxic if swalloed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H413May cause long lasting harmful effects to aquatic life

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P273Avoid release to the environment.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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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

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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:

Capivasertib Amino alcohol Aspartate aminotransferase Ketanserin LDN-193189 HCl RS-127445

  • 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
  • RS-127445, 10 mM in DMSO
  • 199864-87-4
  • 199864-87-3
  • C17H17ClFN3
  • C17H16FN3HCl
  • Inhibitors