TSHR antagonist S37a
Modify Date: 2024-01-08 15:13:44
TSHR antagonist S37a structure
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Common Name | TSHR antagonist S37a | ||
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| CAS Number | 2143452-20-2 | Molecular Weight | 460.57 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C25H20N2O3S2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of TSHR antagonist S37aTSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy[1]. |
| Name | TSHR antagonist S37a |
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| 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 |
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| Molecular Weight | 460.57 |