ML224(NCGC00242364; ANTAG3) is a thyroid-stimulating hormone receptor TSHR counter-agonist with an IC50 of 2.3uM.
| Molecular Weight | 525.59 |
| Formula | C31H31N3O5 |
| CAS Number | 1338824-21-7 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
| Related TSH Receptor Products |
|---|
| D3-βArr
D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro. |
| Org41841
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. |
| VA-K-14 hydrochloride
VA-K-14 hydrochloride is a specific thyroid-stimulating hormone receptor (TSHR) antagonist (IC50= 12.3 μM). |
| ML-109
ML-109 is a full agonist of TSHR (thyroid stimulating hormone receptor) with an EC50 of 40 nM. |
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