产品
编 号：F370652
分子式：C24H30N6O3S2
分子量：514.66
分子式：C24H30N6O3S2
分子量：514.66
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CAS No: 501444-88-8
产品详情
生物活性：
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 EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine.
体内研究：
Org 43553 (5-50 mg/kg; p.o. once) triggers ovulation in immature mice and increases ovulation in GnRH-antagonist-treated rats.Org 43553 (10-250 mg/kg; p.o. once) increases testosterone levels in male rats.1.19Pharmacokinetic Properties of Org 43553 in Rats and Dogs.RatsIV 5 mg/kg RatsPO 50 mg/kgDogsIV 12.5 mg/kg DogsPO 50 mg/kg
AUC (h mg/L)6.9±0.455.1±2.09.1±3.116.1±1.2
Tmax (h) 3.3±3.30.9±1.0
Cmax (mg/L)5.1±2.33.8±0.98.7±2.24.1±1.7
t1/2 (h)3.4±1.34.5±1.81.5±1.33.5±2.5
CL (L/h)0.7±0.10.9±0.11.5±0.63.1±0.2
Animal Model:Immature Humegon primed mice and GnRH-antagonist-treated female Orga rats
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
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.
体外研究：
Org 43553 (0-3 μM; 4 h) shows agonistic activity to human LH, FSH and TSH receptors.
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 EC50 values of 3.7 and 110 nM, respectively. Org 43553 can be used for the research of endocrine.
体内研究：
Org 43553 (5-50 mg/kg; p.o. once) triggers ovulation in immature mice and increases ovulation in GnRH-antagonist-treated rats.Org 43553 (10-250 mg/kg; p.o. once) increases testosterone levels in male rats.1.19Pharmacokinetic Properties of Org 43553 in Rats and Dogs.RatsIV 5 mg/kg RatsPO 50 mg/kgDogsIV 12.5 mg/kg DogsPO 50 mg/kg
AUC (h mg/L)6.9±0.455.1±2.09.1±3.116.1±1.2
Tmax (h) 3.3±3.30.9±1.0
Cmax (mg/L)5.1±2.33.8±0.98.7±2.24.1±1.7
t1/2 (h)3.4±1.34.5±1.81.5±1.33.5±2.5
CL (L/h)0.7±0.10.9±0.11.5±0.63.1±0.2
Animal Model:Immature Humegon primed mice and GnRH-antagonist-treated female Orga rats
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
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.
体外研究：
Org 43553 (0-3 μM; 4 h) shows agonistic activity to human LH, FSH and TSH receptors.
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