2143452-20-2
2143452-20-2 structure
- Name: TSHR antagonist S37a
- Chemical Name: TSHR antagonist S37a
- CAS Number: 2143452-20-2
- Molecular Formula: C25H20N2O3S2
- Molecular Weight: 460.57
- Catalog: Signaling Pathways GPCR/G Protein TSH Receptor
- Create Date: 2020-01-23 20:20:51
- Modify Date: 2024-01-08 15:13:44
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TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1].
| Name | TSHR antagonist S37a |
|---|
| Description | TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1]. |
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| Related Catalog | |
| Target |
TSHR[1] |
| In Vitro | TSHR antagonist S37a exhibits inhibition activity for TSHR, with IC50s of 40 µM and approximately 20 µM for mTSHR and hTSHR, respectively, in HEK293 cells[1]. TSHR antagonist S37a not only inhibits the TSHR activation by thyrotropin itself but also activation by monoclonal TSAb M22 (human), KSAb1 (murine), and the allosteric small-molecule agonist C2[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. |
| References |
| Molecular Formula | C25H20N2O3S2 |
|---|---|
| Molecular Weight | 460.57 |