2. Org 43553

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.

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Org 43553 Chemical Structure

Org 43553 Chemical Structure

CAS No. : 501444-88-8

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Org 43553 Related Antibodies

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Description

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 Vitro

Org 43553 (0-3 μM; 4 h) shows agonistic activity to human LH, FSH and TSH receptors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Org 43553 Related Antibodies

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 EC50 values of 3.7 nM, 110 nM and ＞3 μM, respectively. Showed no CRF1-R agonistic effect in CHO-CRF1 cell line.
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

514.66

Formula

C24H30N6O3S2
CAS No.
SMILES

O=C(C1=C(N)C2=C(C3=CC=CC(NC(CN4CCOCC4)=O)=C3)N=C(SC)N=C2S1)NC(C)(C)C
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Keywords:

Org 43553501444-88-8Org43553Org-43553Inhibitorinhibitorinhibit

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