| Identification | Back Directory | [Name]
Thieno[2,3-d]pyrimidine-6-carboxamide, 5-amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]- | [CAS]
501444-88-8 | [Synonyms]
Org 43553
ORG 43553 HCl
Thieno[2,3-d]pyrimidine-6-carboxamide, 5-amino-N-(1,1-dimethylethyl)-2-(methylthio)-4-[3-[[2-(4-morpholinyl)acetyl]amino]phenyl]- | [Molecular Formula]
C24H30N6O3S2 | [MOL File]
501444-88-8.mol | [Molecular Weight]
514.66 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
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 | | Tmax (h) | | 3.3±3.3 | | 0.9±1.0 | | Cmax (mg/L) | 5.1±2.3 | 3.8±0.9 | 8.7±2.2 | 4.1±1.7 | | t1/2 (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. |
| [References]
[1] van de Lagemaat R, et al. Induction of ovulation by a potent, orally active, low molecular weight agonist (Org 43553) of the luteinizing hormone receptor. Hum Reprod. 2009 Mar;24(3):640-8. DOI:10.1093/humrep/den412 |
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