5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE

Product Name: 5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE
CAS No.: 263847-55-8
Chemical Name: 5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE
Synonyms: AG 045572;5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE;5-((3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl)-N-(2,4,6-trimethoxyphenyl)furan-2-carboxamide;2-Furancarboxamide, 5-[(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)methyl]-N-(2,4,6-trimethoxyphenyl)-
CBNumber: CB32448702
Molecular Formula: C30H37NO5
Formula Weight: 491.62
MOL File: 263847-55-8.mol

More

Less

5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE Property

storage temp.: Store at RT
solubility: <49.16mg/ml in DMSO; <24.58mg/ml in ethanol
form: solid
color: White

More

Less

Hazard and Precautionary Statements (GHS)

More

Less

N-Bromosuccinimide Price

Tocris

Product number: 2730
Product name: AG045572
Purity: ≥97%(HPLC)
Packaging: 1
Price: $112
Updated: 2021/12/16

TRC

Product number: A427023
Product name: AG045572
Packaging: 2.5mg
Price: $330
Updated: 2021/12/16

Usbiological

Product number: 254555
Product name: AG 045572
Packaging: 1mg
Price: $360
Updated: 2021/12/16

ApexBio Technology

Product number: B7163
Product name: AG045572
Packaging: 10mg
Price: $371
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: API0009830
Product name: AG 045572
Purity: 95.00%
Packaging: 5MG
Price: $502.44
Updated: 2021/12/16

More

Less

5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE Chemical Properties,Usage,Production

Uses

AG 045572 is a nonpeptidic GnRH antagonist and has the potential as an oral therapeutic treatement for sex hormone-dependent diseases and infertility.

Biological Activity

Selective gonadotropin-releasing hormone (GnRH) receptor antagonist (K i values are 2.2, 3.8 and 6.0 nM for mouse, rat and human receptors respectively). Suppresses testosterone and luteinising hormone (LH) levels in vivo .

in vivo

AG-045572 (10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time) give to intact male rats, it showed medium T_1/2, CL and V_ss but oral bioavailability was low, in female rats the bioavailability was much higher (24%), in castrated male rats the pharmacokinetics was similar to that in female rats^[1].
AG-045572 (40 mg/kg, i.m. twice a day for 3 days) pretreated of intact male rats resulted in a change of its pharmacokinetics, the parameters became similar to those in female and castrated male rats^[1].
Pharmacokinetic Parameters of AG-045572 in Rats after Administration at 10 mg/kg i.v. and 20 mg/kg p.o.^[1]

Pharmacokinetic Analysis^[1]

Animals	t_1/2 (h)	CL (L/h/kg)	V_ss (L/kg)	C_max (μM)	T_max (h)	F_p.o. (%)
Male	1.4 ± 0.1	2.2 ± 0.5	2.1 ± 0.1	0.61 ± 0.21	1	8
Female	1.7 ± 0.1	1.5 ± 0.1	2.7 ± 0.4	2.31 ± 0.57	1	24
Castrated male	1.7 ± 0.4	1.5 ± 0.3	3.7 ± 1.5	1.98 ± 0.51	1	23
Pretreated male	1.9 ± 0.2	1.5 ± 0.2	2.0 ± 0.6	1.89 ± 0.41	1	27

Animal Model:	Male rats were surgically castrated via scrotal approach under halothane anesthesia and allowed 14 days post-operative recovery prior to study^[1]
Dosage:	10 mg/kg, 20 mg/kg; 40 mg/kg
Administration:	administered acutely at 10 mg/kg (i.v.) or 20 mg/kg (p.o.), one time; For multiple-dose pretreatment, male rats at 40 mg/kg, i.m. twice a day for 3 days.
Result:	Showed medium T_1/2, CL and V_ss but oral bioavailability was low, in female rats the bioavailability was much higher (24%) Became similar to those in female and castrated male rats.

References

[1]. barnes mj, burschka c, büttner mw, et al. silicon analogues of the nonpeptidic gnrh antagonist ag-045572: syntheses, crystal structure analyses, and pharmacological characterization. chemmedchem, 2011, 6(11): 2070-2080.
[2]. zhu yf, chen c, struthers rs. nonpeptide gonadotropin releasing hormone antagonists. annu. rep. med. chem, 2004, 39(99): 110.
[3]. anderes kl, luthin dr, castillo r, et al. biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (gnrh) antagonist using castrated and intact rats. journal of pharmacology and experimental therapeutics, 2003, 305(2): 688-695.
[4]. herbst kl. gonadotropin-releasing hormone antagonists. current opinion in pharmacology, 2003, 3(6): 660-666.

5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE Preparation Products And Raw materials

Raw materials

Preparation Products

More

Less

5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE Suppliers

China 31 United Kingdom 1 United States 5 USA 1 Global 38

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

Tel: 821-50328103-801 18930552037
Fax: 86-21-50328109
Email: 3bsc@sina.com
Country: China
ProdList: 15838
Advantage: 69

Bide Pharmatech Ltd.

Tel: 400-164-7117 13681763483
Fax: +86-21-61629029
Email: product02@bidepharm.com
Country: China
ProdList: 39966
Advantage: 60

Shanghai EFE Biological Technology Co., Ltd.

Tel: 021-65675885 18964387627
Fax: 021-65675885
Email: info@efebio.com
Country: China
ProdList: 9803
Advantage: 58

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
Advantage: 60

Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
ProdList: 9125
Advantage: 58

Jinan ponder chemical co. LTD

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

Wuhan Topule

Tel: +86-02787215551 +86-19945035818
Fax: 027-87215551
Email: 2936752263@qq.com
Country: China
ProdList: 7986
Advantage: 58

Beijing Biocreative Technology Co., Ltd.

Tel: 15522676233
Email: 3007606172@qq.com
Country: China
ProdList: 1248
Advantage: 58

TargetMol Chemicals Inc.

Tel: 4008200310
Email: marketing@tsbiochem.com
Country: China
ProdList: 24961
Advantage: 58

Nantong QuanYi Biotechnology Co., Ltd

Tel: 0513-66337626 18051384581
Email: sales@chemhifuture.com
Country: China
ProdList: 5929
Advantage: 58

Shanghai Aladdin Biochemical Technology Co.,Ltd.

Tel: 400-6206333 13167063860
Email: anhua.mao@aladdin-e.com
Country: China
ProdList: 48457
Advantage: 58

Shanghai Fine Biotech Co.，Ltd

Tel: 18221172427
Email: sale@fine-biotech.com
Country: China
ProdList: 2760
Advantage: 58

Sangon Biotech (Shanghai) Co.,Ltd.

Tel: 400-821-026
Email: Sales@sangon.com
Country: China
ProdList: 6710
Advantage: 58

Cayman Chemical Company

Tel: 800-364-9897
Email: sales@caymanchem.com
Country: China
ProdList: 6838
Advantage: 58

Santa Cruz Biotechnology Inc

Tel: 021-60936350
Email: scbt@scbt.com
Country: China
ProdList: 6594
Advantage: 58

ATK CHEMICAL COMPANY LIMITED

Tel: +undefined-21-51877795
Fax: +86 21 5161 9052/ 5187 7796
Email: ivan@atkchemical.com
Country: China
ProdList: 33024
Advantage: 60

Wuhan Topule Biopharmaceutical Co., Ltd

Tel: +8618327326525
Email: masar@topule.com
Country: China
ProdList: 8467
Advantage: 58

Hangzhou MolCore BioPharmatech Co.,Ltd.

Tel: +86-057181025280; +8617767106207
Fax: 0571-85806285
Email: sales@molcore.com
Country: China
ProdList: 49734
Advantage: 58

Chongqing Boer Biotechnology Co., Ltd.

Tel: 13251428727， 13368356747
Country: CHINA
ProdList: 157
Advantage: 58

Dibai Biotechnology (Nanjing) Co., Ltd.

Tel: 025-58649515
Country: CHINA
ProdList: 190
Advantage: 58

Guangzhou Tuoshan Biotechnology Co., Ltd.

Tel: 19928332050
Country: CHINA
ProdList: 161
Advantage: 58

Guangzhou Suyan Biotechnology Co., Ltd

Tel: 18818417021
Country: CHINA
ProdList: 127
Advantage: 58

Absin Bioscience Inc.

Tel: --
Fax: --
Email: chenjw@absin.cn
Country: CHINA
ProdList: 6208
Advantage: 58

Proteintech China

Tel: --
Fax: --
Email: Proteintech-CN@ptglab.com
Country: CHINA
ProdList: 6290
Advantage: 58

Beijing Taize Jiaye Technology Development Co., Ltd.

Tel: --
Fax: --
Country: CHINA
ProdList: 6050
Advantage: 58

Beijing Bolide Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: 1985563437@qq.com
Country: CHINA
ProdList: 6525
Advantage: 58

Shanghai Weiwei Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: sales@wheybio.com
Country: CHINA
ProdList: 4398
Advantage: 58

Shanghai Gantu Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: 1920192055@qq.com
Country: CHINA
ProdList: 1843
Advantage: 58

Shanghai Haoyang Biological Technology Co., Ltd.

Tel: --
Fax: --
Email: 596799915@QQ.COM
Country: CHINA
ProdList: 2905
Advantage: 58

Shanghai Yihui Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: yihbio@163.com
Country: CHINA
ProdList: 6184
Advantage: 58

Shanghai Chaoyan Biotechnology Co., Ltd.

Tel: --
Fax: --
Email: 471161314@qq.com
Country: CHINA
ProdList: 6210
Advantage: 58

263847-55-8, 5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDERelated Search:

3,5-DIMETHOXY-2-AMINO-PHENOL 5-BENZYL-2-FURALDEHYDE 5-(4-METHYLBENZYL)-2-FURALDEHYDE N-(2,6-DIMETHOXYPHENYL)ACETAMIDE 2,4,6-TRIMETHOXYANILINE CHEMBRDG-BB 7994587 5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE

5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE

AG 045572

2-Furancarboxamide, 5-[(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)methyl]-N-(2,4,6-trimethoxyphenyl)-

5-((3,5,5,8,8-Pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl)-N-(2,4,6-trimethoxyphenyl)furan-2-carboxamide

263847-55-8