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

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

Less

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

Less

Hazard and Precautionary Statements (GHS)

Less

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

Less

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-HT_2B (K_i = 0.32 nM). It is selective for 5-HT_2B over other 5-HT receptor subtypes (K_i = >3 μM for 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C, 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

Less

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

China 88 India 2 United Kingdom 2 United States 15 Global 107

Shanghai Boyle Chemical Co., Ltd.

Tel
Fax: 86-21-57758967
Email: sales@boylechem.com
Country: China
ProdList: 2922
Advantage: 55

3B Pharmachem (Wuhan) International Co.,Ltd.

Tel: 821-50328103-801 18930552037
Fax: 86-21-50328109
Email: 3bsc@sina.com
Country: China
ProdList: 15839
Advantage: 69

Shanghai civi chemical technology co.,Ltd

Tel: 86-21-34053660
Fax: 86-21-34053661
Email: sale@labgogo.com
Country: China
ProdList: 9865
Advantage: 52

NCE Biomedical Co.,Ltd.

Tel: 4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax: +86-27-87599188
Country: China
ProdList: 1493
Advantage: 55

Suzhou yacoo science co.,Ltd

Tel: 0512-87182056 18013166090
Fax: 0512-87182056
Email: lingling.qi@yacoo.com.cn
Country: China
ProdList: 7295
Advantage: 60

AdooQ Bioscience CHINA

Tel: 025-58849295 18951903616;
Fax: 025-68650336
Email: info@adooq.cn
Country: China
ProdList: 2990
Advantage: 60

LETOPHARM LIMITED

Tel: +86-21-5821 5861
Fax: +86-21-5106 2861
Email: sales@letopharm.com
Country: China
ProdList: 2384
Advantage: 58

Shanghaizehan biopharma technology co., Ltd.

Tel: 021-61350663 13052117465
Fax: 021-61350662
Email: sales@zehanbiopharma.com
Country: China
ProdList: 1009
Advantage: 55

DebyeTec.com Inc.

Tel: 18086626237 18086626237
Fax: qq:2693528373
Email: sales@debyesci.com
Country: China
ProdList: 2645
Advantage: 56

D&C Chemicals

Tel: +86-21-58447131
Fax: +86-21-61642470
Email: 1724405207@qq.com
Country: China
ProdList: 472
Advantage: 55

SPIRO PHARMA

Tel
Fax: -
Email: eric_feng1954@126.com
Country: China
ProdList: 9248
Advantage: 55

CHMA Chemical Technology (Shanghai) Co., Ltd

Tel: 021-61556450 15800904410
Fax: 021-61556450
Country: China
ProdList: 2832
Advantage: 58

Codow Chemical Co.,Ltd.

Tel: 18620099427
Fax: +86-20-62619665
Email: amy@howeipharm.com
Country: China
ProdList: 17687
Advantage: 55

Guangzhou QiYun Biotechnology Co., Ltd.

Tel: 020-61288194 61288195
Fax: 020-61288700
Email: 505721671@qq.com
Country: China
ProdList: 3866
Advantage: 58

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 27313
Advantage: 60

Tianjin Kailiqi Biotechnology Co., Ltd.

Tel: 15076683720
Fax: 022-23754520
Email: klq@cw-bio.com
Country: China
ProdList: 4600
Advantage: 55

ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8011
Advantage: 62

Amadis Chemical Company Limited

Tel: 571-89925085
Fax: 0086-571-89925065
Email: sales@amadischem.com
Country: China
ProdList: 131957
Advantage: 58

Beijing Jin Ming Biotechnology Co., Ltd.

Tel: 010-60605840 18892239720
Fax: 010-60605840
Email: psaitong@jm-bio.com
Country: China
ProdList: 12306
Advantage: 58

Hefei Hirisun Pharmatech Co., Ltd.

Tel: +86-0551-62678551 +86-15056975894
Fax: 0551-62678551
Email: sales@hirisunpharm.com
Country: China
ProdList: 181
Advantage: 55

Shanghai Biopharmaleader Co., Ltd.

Tel: +86 18721201413
Fax: +86 (21) 5775-8967
Email: sales@biopharmaleader.com
Country: China
ProdList: 1720
Advantage: 58

Amatek Scientific Co. Ltd.

Tel: 0512-56316828
Fax: 0512-56316826
Email: info@amateksci.com
Country: China
ProdList: 28806
Advantage: 58

Aikon International Limited

Tel: 025-58851090 13611564524
Fax: (6)02557626880
Email: lwan@aikonchem.com
Country: China
ProdList: 15951
Advantage: 58

Hefei zhongxing Biomedical Co., Ltd.

Tel: 15955174703
Fax: -
Email: 149498276@qq.com
Country: China
ProdList: 80
Advantage: 58

Angel Pharmatech, Ltd.

Tel: 17317130613
Fax: QQ3358272972
Email: 3358272972@qq.com
Country: China
ProdList: 3251
Advantage: 58

Guangzhou Tomums Life Science Co., Ltd.

Tel: 020-31155029 18902330969
Fax: 020-31155029
Email: sales@tomums.cn
Country: China
ProdList: 4696
Advantage: 58

Zhejiang Zetian Fine Chemical Co., Ltd.

Tel: 0571-87682782 18957127338
Fax: QQ800182836
Email: sales@zetchem.com
Country: China
ProdList: 569
Advantage: 58

Taizhou Crene Biotechnology Co. Ltd.

Tel: +86-0576-88813233 +86-13396860566
Email: sales@pharm-intermediates.com
Country: China
ProdList: 1990
Advantage: 58

Hefei Hirisun Pharmatech Co., Ltd

Tel: +8615056975894
Fax: 86-0551-62678551
Email: shawn@hirisunpharm.com
Country: CHINA
ProdList: 9911
Advantage: 58

Dideu Industries Group Limited

Tel: +86-29-89586680 +86-15129568250
Email: 1026@dideu.com
Country: China
ProdList: 22883
Advantage: 58

Hubei Jusheng Technology Co.,Ltd.

Tel: 18871490254
Fax: 027-59599243
Email: linda@hubeijusheng.com
Country: CHINA
ProdList: 28172
Advantage: 58

DC Chemicals

Tel: 021-58447131 13564518121
Email: sales@dcchemicals.com
Country: China
ProdList: 9409
Advantage: 58

Guangdong Wengjiang Chemical Reagent Co., Ltd.

Tel: 0751-2886766 13927870850
Fax: 0751-2886756
Email: 3001267247@qq.com
Country: China
ProdList: 9974
Advantage: 58

Jinan ponder chemical co. LTD

Tel: 0531-0000
Email: thinklifescience@163.com
Country: China
ProdList: 19689
Advantage: 58

Shanghai Yanze Chemical Co., Ltd.

Tel: 021-13773155751 19975051755
Email: 260924549@qq.com
Country: China
ProdList: 8904
Advantage: 58

CONIER CHEM AND PHARMA LIMITED

Tel: +8618523575427
Email: sales@conier.com
Country: China
ProdList: 49374
Advantage: 58

career henan chemical co

Tel: +86-0371-86658258 +8613203830695
Fax: 0086-371-86658258
Email: factory@coreychem.com
Country: China
ProdList: 29811
Advantage: 58

Absin Bioscience Inc.

Tel: 021-38015121 15000105423
Email: wulan@absin.cn
Country: China
ProdList: 24731
Advantage: 58

Shanghai hongqu biomedical technology co. LTD

Tel: 88888888888
Email: hongquchem@qq.com
Country: China
ProdList: 5132
Advantage: 58

Wuhan Yanzhe Technology Co., Ltd

Tel: 15527250409
Fax: QQ：2692360204
Email: wenhaotian12@163.com
Country: China
ProdList: 4495
Advantage: 58

MedBioPharmaceutical Technology Inc

Tel: 021-69568360 18916172912
Email: order@med-bio.cn
Country: China
ProdList: 8140
Advantage: 58

Energy Chemical

Tel: 021-58432009 400-005-6266
Fax: 021-58436166
Email: marketing@energy-chemical.com
Country: China
ProdList: 44918
Advantage: 58

cjbscvictory

Tel: 13348960310 13348960310
Email: 3003867561@qq.com
Country: China
ProdList: 10002
Advantage: 58

Abmole Bioscience Inc.

Tel: 021-50967598 02150967598
Email: sales@abmole.cn
Country: China
ProdList: 4494
Advantage: 58

Shanghai tingchong biology science and technology co., ltd

Tel: 18964309092 18964309092
Email: 2769493375@qq.com
Country: China
ProdList: 2634
Advantage: 58

Shanghai Universal Biotech Co.,Ltd

Tel: 13774214275
Email: zhouzz@univ-bio.com
Country: China
ProdList: 24990
Advantage: 58

Hubei Kele Fine Chemical Co., Ltd

Tel: 027-59101668 19945030958
Fax: 027-59101668
Email: 2881924765@qq.com
Country: China
ProdList: 8099
Advantage: 58

Bide Pharmatech Ltd.

Tel: 400-1647117 13681763483
Email: product02@bidepharm.com
Country: China
ProdList: 62075
Advantage: 58

InvivoChem

Tel: 13549236410
Email: sales@invivochem.cn
Country: China
ProdList: 6753
Advantage: 58

Wuhan Yingnuo Pharmaceutical Technology Co., Ltd.

Tel: +86-027-59232304 15387063101
Email: 2881924050@qq.com
Country: China
ProdList: 9953
Advantage: 58

Less

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:

Amino alcohol Aspartate aminotransferase Ketanserin AZD5363 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

199864-87-4

199864-87-3

C17H17ClFN3

C17H16FN3HCl

Inhibitors