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

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
Molecular Weight:
281.33
MDL Number:
MFCD20270616
MOL File:
199864-87-4.mol
Last updated:2024-11-19 23:02:33

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

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
FDA UNII 0JAU3P8OBM

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE price More Price(33)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 23451 RS 127445 ≥98% 199864-87-4 1mg $28 2022-04-27 Buy
Cayman Chemical 23451 RS 127445 ≥98% 199864-87-4 5mg $96 2022-04-27 Buy
Cayman Chemical 23451 RS 127445 ≥98% 199864-87-4 10mg $177 2022-04-27 Buy
Tocris 2993 RS-127445 hydrochloride ≥98%(HPLC) 199864-87-4 50 $820 2021-12-16 Buy
Tocris 2993 RS-127445 hydrochloride ≥98%(HPLC) 199864-87-4 10 $203 2021-12-16 Buy
Product number Packaging Price Buy
23451 1mg $28 Buy
23451 5mg $96 Buy
23451 10mg $177 Buy
2993 50 $820 Buy
2993 10 $203 Buy

4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE Chemical Properties,Uses,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

Global( 107)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32957 60
Zhejiang ZETian Fine Chemicals Co. LTD
+8618957127338 stella@zetchem.com China 2136 58
Hubei Jusheng Technology Co.,Ltd.
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CONIER CHEM AND PHARMA LIMITED
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career henan chemical co
+86-0371-86658258 +8613203830695 factory@coreychem.com China 29811 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 32165 58
Dideu Industries Group Limited
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Hefei Hirisun Pharmatech Co., Ltd
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InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
Henan Aochuang Chemical Co.,Ltd.
+86-0371-63689365 +8618638391208 sales@aochuangchem.com China 9237 58

View Lastest Price from 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
RS-127445 pictures 2024-11-19 RS-127445
199864-87-4
US $46.00-142.00 / mg 98.81% 10g TargetMol Chemicals Inc.
2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine pictures 2022-09-08 2-amino-4-(4-fluoronaphth-1-yl)-6-isopropylpyrimidine
199864-87-4
US $0.00-0.00 / kg 1kg 98% 1Ton Henan Aochuang Chemical Co.,Ltd.
4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE pictures 2020-01-09 4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE
199864-87-4
US $3.00 / KG 1KG 98% 200KG Career Henan Chemical Co
  • RS-127445 pictures
  • RS-127445
    199864-87-4
  • US $46.00-142.00 / mg
  • 98.81%
  • TargetMol Chemicals Inc.

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

199864-87-4(4-(4-FLUORO-1-NAPHTHALENYL)-6-(1-METHYLETHYL)-2-PYRIMIDINAMINE HYDROCHLORIDE)Related 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 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 445 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