Product Name :
TSHR antagonist S37a
Description:
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves’ orbitopathy.
CAS:
2143452-20-2
Molecular Weight:
459.56
Formula:
C25H19N2O3S2
Chemical Name:
(1S,2S,10R,11R,12R,16R)-6,13,15-trioxo-9,14-diphenyl-3,7-dithia-5,14-diazapentacyclo[9.5.1.0²,¹⁰.0⁴,⁸.0¹²,¹⁶]heptadec-4(8)-en-9-yl
Smiles :
O=C1[C@@H]2[C@H]3C[C@H]([C@@H]4SC5NC(=O)SC=5[C]([C@@H]43)C3C=CC=CC=3)[C@@H]2C(=O)N1C1C=CC=CC=1 |^1:14|
InChiKey:
LIXLPTOYTCDPJN-BEUOHLRXSA-N
InChi :
InChI=1S/C25H19N2O3S2/c28-23-18-14-11-15(19(18)24(29)27(23)13-9-5-2-6-10-13)20-17(14)16(12-7-3-1-4-8-12)21-22(31-20)26-25(30)32-21/h1-10,14-15,17-20H,11H2,(H,26,30)/t14-,15-,17-,18+,19-,20-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves’ orbitopathy.|Product information|CAS Number: 2143452-20-2|Molecular Weight: 459.56|Formula: C25H19N2O3S2|Chemical Name: (1S,2S,10R,11R,12R,16R)-6,13,15-trioxo-9,14-diphenyl-3,7-dithia-5,14-diazapentacyclo[9.5.1.0²,¹⁰.0⁴,⁸.0¹²,¹⁶]heptadec-4(8)-en-9-yl|Smiles: O=C1[C@@H]2[C@H]3C[C@H]([C@@H]4SC5NC(=O)SC=5[C]([C@@H]43)C3C=CC=CC=3)[C@@H]2C(=O)N1C1C=CC=CC=1 |^1:14||InChiKey: LIXLPTOYTCDPJN-BEUOHLRXSA-N|InChi: InChI=1S/C25H19N2O3S2/c28-23-18-14-11-15(19(18)24(29)27(23)13-9-5-2-6-10-13)20-17(14)16(12-7-3-1-4-8-12)21-22(31-20)26-25(30)32-21/h1-10,14-15,17-20H,11H2,(H,26,30)/t14-,15-,17-,18+,19-,20-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 100 mg/mL (217.{{EGF Protein, Human} MedChemExpress|{EGF Protein, Human} Biological Activity|{EGF Protein, Human} Formula|{EGF Protein, Human} custom synthesis|{EGF Protein, Human} Autophagy} 12 mM; Need ultrasonic).{{Tofisopam} medchemexpress|{Tofisopam} Technical Information|{Tofisopam} Purity|{Tofisopam} custom synthesis|{Tofisopam} Cancer} |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:26446225 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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. 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.|In Vivo:|TSHR antagonist S37a also inhibits cyclic adenosine monophosphate formation by oligoclonal TSAb, which are highly enriched in GO patients’ sera. TSHR antagonist S37a (10 mg/kg ;i.g.) displays no toxicity and a remarkable 53% oral bioavailability in mice.|Products are for research use only. Not for human use.|
