Org 43553 是一种具有口服活性的低分子量 (LMW) 促黄体生成素受体(LH-R)激动剂。Org 43553 对人 LH 和 FSH 受体具有激动作用，其EC50值分别为 3.7 nM 和 110 nM。Org 43553 可以用于内分泌的研究。

Org 43553 is an orally active and low molecular weight (LMW) luteinizing hormone receptor (LH-R) agonist. Org 43553 shows agonistic activity to human LH and FSH receptors with EC 50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine [1].

Org 43553 (0-3 μM; 4 h) shows agonistic activity to human LH, FSH and TSH receptors [1]. Cell Viability Assay [1] Cell Line: CHO and HEK293 cell lines Concentration: 0-3 μM Incubation Time: 4 hours Result: Exhibited agonistic activity to human LH, FSH and TSH receptors with EC 50 values of 3.7 nM, 110 nM and ＞3 μM, respectively. Showed no CRF1-R agonistic effect in CHO-CRF1 cell line.

Org 43553 (5-50 mg/kg; p.o. once) triggers ovulation in immature mice and increases ovulation in GnRH-antagonist-treated rats [1]. Org 43553 (10-250 mg/kg; p.o. once) increases testosterone levels in male rats [1]. 1.19 Pharmacokinetic Properties of Org 43553 in Rats and Dogs [1]. Rats IV 5 mg/kg Rats PO 50 mg/kg Dogs IV 12.5 mg/kg Dogs PO 50 mg/kg AUC (h mg/L) 6.9±0.4 55.1±2.0 9.1±3.1 16.1±1.2 T max (h) 3.3±3.3 0.9±1.0 C max (mg/L) 5.1±2.3 3.8±0.9 8.7±2.2 4.1±1.7 t 1/2 (h) 3.4±1.3 4.5±1.8 1.5±1.3 3.5±2.5 CL (L/h) 0.7±0.1 0.9±0.1 1.5±0.6 3.1±0.2 Animal Model: Immature Humegon primed mice and GnRH-antagonist-treated female Orga rats [1] Dosage: 5-50 mg/kg Administration: Oral gavage; 50 mg/kg once Result: Triggered ovulation in 80% of the animals, with a mean number of 9.3 ova per ovulating animals. Dose-dependently increased the number of ovulated oocytes in the ampulla, and showed a similar ovulation number at a dose of 25 mg/kg compared with hCG group. Animal Model: Adult male rats [1] Dosage: 10, 50 and 250 mg/kg Administration: Oral gavage; 10-250 mg/kg once Result: Significantly increased testosterone production in male rats and at a dose of 250 mg/kg the testosterone levels were very similar to those induced by hCG.

501444-88-8

C24H30N6O3S2

514.66

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years