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Org41841 

Cat. No. M29864
Org41841  Structure
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Biological Activity

Org41841 is a partial agonist of both luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and thyroid-stimulating hormone receptor (TSHR) with EC50s of 0.2 and 7.7 μM, respectively.

Chemical Information
Molecular Weight 402.53
Formula C19H22N4O2S2
CAS Number 301847-37-0
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Claire L Newton, et al. Handb Exp Pharmacol. Pharmacoperones for Misfolded Gonadotropin Receptors

[2] Jo Ann Janovick, et al. Mol Cell Endocrinol. Increased plasma membrane expression of human follicle-stimulating hormone receptor by a small molecule thienopyr(im)idine

[3] Susanne Neumann, et al. Endocrinology. A low-molecular-weight antagonist for the human thyrotropin receptor with therapeutic potential for hyperthyroidism

[4] Susanna Moore, et al. J Med Chem. Evaluation of small-molecule modulators of the luteinizing hormone/choriogonadotropin and thyroid stimulating hormone receptors: structure-activity relationships and selective binding patterns

[5] Holger Jäschke, et al. J Biol Chem. A low molecular weight agonist signals by binding to the transmembrane domain of thyroid-stimulating hormone receptor (TSHR) and luteinizing hormone/chorionic gonadotropin receptor (LHCGR)

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