| CAS NO: | 263847-55-8 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 10mg | 电议 |
| Cas No. | 263847-55-8 |
| 化学名 | 5-((3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)methyl)-N-(2,4,6-trimethoxyphenyl)furan-2-carboxamide |
| Canonical SMILES | O=C(C1=CC=C(CC2=C(C)C=C3C(C)(C)CCC(C)(C)C3=C2)O1)NC(C(OC)=CC(OC)=C4)=C4OC |
| 分子式 | C30H37NO5 |
| 分子量 | 491.62 |
| 溶解度 | <49.16mg/ml in DMSO;<24.58mg/ml in ethanol |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | AG 045572, also called CMPD1, is a nonpeptidic antagonist of gonadotropin-releasing hormone (GnRH) [1], with Ki values of 6.0 nM and 2.2nM to human and mouse GnRH receptors, respectively [2]. GnRH is a neuroendocrine decapeptide (pGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro- Gly-NH2). It is synthesized in the neurovascular terminals of the hypothalamus and hence secreted directly into the hypophyseal portal blood supply in a pulsatile manner. GnRH selectively binds specific receptors on membranes of anterior pituitary gonadotroph cells to stimulate the synthesis and the release of the gonadotropic hormones [follicle-stimulating hormone (FSH) and luteinizing hormone (LH)]. FSH and LH stimulate gametogenesis and gonadal production of sex steroids, respectively [3]. In 293 cells expressing human GnRH receptors, GnRH concentration-dependently increased the accumulation of total [3H] inositol phosphate. This response to GnRH showed an EC50 value of 0.6 ± 0.15 nM (n = 10) with a Hill coefficient of 0.98 ± 0.05. AG 045572 alone did not produce any change in basal levels of inositol phosphates. But AG 045572 concentration-dependently inhibited the response to GnRH. The mean KB ± S.E. of six similar experiments was 25 ± 0.9 nM for AG 045572 at the human receptor. TRH concentration-dependently stimulate the accumulation of total inositol phosphate in GGH3 cells with an EC50 value of 2.4 ± 0.16. AG 045572 at concentrations up to 10 μM had no appreciable inhibition of the accumulation of inositol phosphate stimulated by TRH [3]. After oral administration with AG 045572 at a single dose of 100mg/kg, the concentration of plasma LH in castrated male rats was completely suppressed up to 8 h. 0.5 h after a single intravenous administration with AG 045572 at 10mg/kg, LH levels were suppressed to almost baseline. But this effect lasted for less than 2 h. AG 045572 at a single intravenous dose of 20 mg/kg also reduced concentrations of testosterone in intact male rats [2]. To intact male rats, administration with AG 045572 at a single dose of 100 mg/kg, maintained the suppression of testosterone in the castrate range for 24 hours [4]. References: |
m.cnreagent.com