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

TSHR antagonist S37a 

Cat. No.: HY-129995A
Handling Instructions

TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.

For research use only. We do not sell to patients.

TSHR antagonist S37a Chemical Structure

TSHR antagonist S37a Chemical Structure

CAS No. : 2143452-20-2

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of TSHR antagonist S37a:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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([[email protected]]2C3=CC=CC=C3)=C1S[[email protected]@]([[email protected]@]2([H])[[email protected]@]4([H])[[email protected]@]56[H])([H])[[email protected]](C4)([H])[[email protected]]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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
TSHR antagonist S37a
Cat. No.:
HY-129995A
Quantity:
MCE Japan Authorized Agent: