SW-106 

SW-106 is a selective antagonist of parathyroid hormone/parathyroid hormone-related peptide receptor (PPR) and PTHR1, with an IC₅₀ value of 0.99 μM against PPR. SW-106 antagonizes cAMP responses. SW-106 can be used in the research of osteoporosis^[1][2].

SW-106 (incubated for 3 h) competes with the PPR probe peptide DPC-AJ1951 for binding to PPR in B28 cells, with an IC₅₀ of 0.99 μM, and does not act as an agonist to induce cAMP production in these cells^[1].
SW-106 acts as a competitive antagonist of PPR-mediated cAMP production in B28, SaOS-2 and UMR106 cells, with an IC₅₀ of 5.78 μM against DPC-AJ1951 and 68 μM against PTH-(1-34) in B28 cells^[1].
SW-106 exhibits more selective activity toward PPR than toward the GLP-1 receptor and most tested class A GPCRs, showing only weak binding to a small subset of class A receptors at concentrations ≥10 μM^[1].
SW-106 (3 × 10^-5 M; up to 90 min) exhibits weak intrinsic agonist activity toward wild-type hPTHR1 expressed in GS-22A cells, increasing cAMP levels by ~5-fold at a concentration of 3 × 10^-5 M^[2].
SW-106 (1 × 10^-6 M-1 × 10^-5 M; up to 30 min) effectively inhibits the cAMP signaling pathway mediated by the tethered PTH (1-9) sequence on PTHR-Tether (1-9) expressed in GS-22A cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

361.31

C₁₇H₁₆F₅NO₂

O=C1NC2=CC=C(F)C(F)=C2[C@](C(F)(F)F)(/C=C/C3CC3)O[C@H]1CC

Room temperature in continental US; may vary elsewhere.

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• [1]. Carter PH, et al. Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe. Proc Natl Acad Sci U S A. 2007 Apr 17;104(16):6846-51.  [Content Brief]

  [2]. Carter PH, et al. Actions of the small molecule ligands SW106 and AH-3960 on the type-1 parathyroid hormone receptor. Mol Endocrinol. 2015;29(2):307-321.  [Content Brief]