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Org 43553 

Cat. No. M30192
Org 43553  Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 514.66
Formula C24H30N6O3S2
CAS Number 501444-88-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] K V Derkach, et al. Tsitologiia. THE STIMULATING EFFECT OF THIENOPYRIMIDINES, THE STRUCTURAL ANALOGS OF ORG 43553, ON THE ACTIVITY OF ADENYLYL CYCLASE IN THE TESTES AND ON THE TESTOSTERONE PRODUCTION IN MALE RATS

[2] Claire L Newton, et al. Handb Exp Pharmacol. Pharmacoperones for Misfolded Gonadotropin Receptors

[3] Mireille Gerrits, et al. J Clin Endocrinol Metab. First evidence of ovulation induced by oral LH agonists in healthy female volunteers of reproductive age

[4] R van de Lagemaat, et al. Hum Reprod. Induction of ovulation by a potent, orally active, low molecular weight agonist (Org 43553) of the luteinizing hormone receptor

[5] Laura H Heitman, et al. Mol Pharmacol. [3H]Org 43553, the first low-molecular-weight agonistic and allosteric radioligand for the human luteinizing hormone receptor

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Keywords: Org 43553  supplier, inhibitors, activators


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