A TSHR allosteric antagonist
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ORG 274179-0

Item No. 43557

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(4S)-1-acetyl-1,2,3,4-tetrahydro-4-methyl-4-phenyl-6-quinolinyl]-3-(trifluoromethyl)-benzenepropanamide
CAS Number
1421683-12-6
Molecular Formula
C28H27F3N2O2
Formula Weight
480.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(NC(C=C12)=CC=C1N(C(C)=O)CC[C@@]2(C)C3=CC=CC=C3)CCC4=CC(C(F)(F)F)=CC=C4
InChi Code
InChI=1S/C28H27F3N2O2/c1-19(34)33-16-15-27(2,21-8-4-3-5-9-21)24-18-23(12-13-25(24)33)32-26(35)14-11-20-7-6-10-22(17-20)28(29,30)31/h3-10,12-13,17-18H,11,14-16H2,1-2H3,(H,32,35)/t27-/m0/s1
InChi Key
IOEFWCOWBKDSQX-MHZLTWQESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $72

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    5 mg

    $323

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    10 mg

    $572

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    25 mg

    $1,073

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    Product Description

    ORG 274179-0 is a thyroid-stimulating hormone receptor (TSHR) allosteric antagonist.1 It inhibits TSHR activation induced by bovine TSH, human TSH, or the TSH-receptor-stimulating immunoglobulin M22 in reporter assays using CHO cells expressing the human receptor (IC50s = 30, 26, and 56 nM, respectively). ORG 274179-0 inhibits bovine TSH- or M22-induced phospholipase C (PLC) activation in CHO cells expressing human TSHR (IC50s = 5 and 4 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. van Koppen, C.J., de Gooyer, M.E., Karstens, W.-J., et al. Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor. Br. J. Pharmacol. 165(7), 2314-2324 (2012).