1. GPCR/G Protein
  2. TSH Receptor
  3. TSHR antagonist S37a

TSHR antagonist S37a 

目录号: HY-129995A
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TSHR antagonist S37a 是一个高选择性的促甲状腺激素受体 TSHR 拮抗剂,具有研究格雷夫斯眼窝病的潜力 。

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TSHR antagonist S37a Chemical Structure

TSHR antagonist S37a Chemical Structure

CAS No. : 2143452-20-2

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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].

IC50 & 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.
Molecular Weight

460.57

Formula

C₂₅H₂₀N₂O₃S₂

CAS No.

2143452-20-2

SMILES

O=C(N1)SC([C@H]2C3=CC=CC=C3)=C1S[C@@]([C@@]2([H])[C@@]4([H])[C@@]56[H])([H])[C@](C4)([H])[C@]6([H])C(N(C7=CC=CC=C7)C5=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

TSHR antagonist S37aTSH ReceptorThyrotropin receptorThyroid-stimulating hormone ReceptorthyrotropinreceptorTSHRantagonistInhibitorinhibitorinhibit

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产品名称:
TSHR antagonist S37a
目录号:
HY-129995A
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