| Identification | Back Directory | [Name]
TSHR antagonist S37a | [CAS]
2143452-20-2 | [Synonyms]
TSHR antagonist S37a
TSHR antagonist S37a,TSHR antagonist S-37a
5,9-Methanothiazolo[5',4':5,6]thiopyrano[2,3-f]isoindole-2,6,8(7H)-trione, 3,4a,5,5a,8a,9,9a,10-octahydro-7,10-diphenyl-, (4aS,5S,5aR,8aR,9R,9aS,10R)- | [Molecular Formula]
C25H20N2O3S2 | [MDL Number]
MFCD33548839 | [MOL File]
2143452-20-2.mol | [Molecular Weight]
460.57 |
| Chemical Properties | Back Directory | [density ]
1.54±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (217.12 mM; Need ultrasonic) | [form ]
Solid | [pka]
9.16±0.40(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1]. | [in vivo]
TSHR antagonist S37a also inhibits cyclic adenosine monophosphate formation by oligoclonal TSAb, which are highly enriched in GO patients' sera[1].
TSHR antagonist S37a (10 mg/kg ;i.g.) displays no toxicity and a remarkable 53% oral bioavailability in mice[1].
| Animal Model: | SWISS (CD1) mice (38-43 g)[1] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage | | Result: | Displays a remarkable 53% oral bioavailability as well as a half‐life of 2.9 hours after oral application. |
| [storage]
Store at -20°C | [References]
[1] Marcinkowski P, et al. A New Highly Thyrotropin Receptor-Selective Small-Molecule Antagonist with Potential for the Treatment of Graves' Orbitopathy. Thyroid. 2019 Jan;29(1):111-123. DOI:10.1089/thy.2018.0349 |
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