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

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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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

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

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

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

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

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

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

P501Dispose of contents/container to..…

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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

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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

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

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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