Ronacaleret hydrochloride  (Synonyms: SB 751689A)

Ronacaleret hydrochloride (SB 751689A) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret hydrochloride (SB 751689A) is used for the study of postmenopausal osteoporosis^[1].

Ronacaleret inhibits OATP1B1 (IC₅₀ = 11 μM) and OATP2B1 (IC₅₀ = 12 μM) in vitro, whereas it does not inhibit BCRP^[3].
Ronacaleret is shown to inhibit the OATP1B1- and OATP1B3-mediated uptake of the probe substrate estradiol-glucuronide with relatively low potency (IC₅₀ values of 11 and 60 μM, respectively)^[3].
Ronacaleret inhibits OATP2B1-mediated rosuvastatin transport at pH 7.4 and pH 6.0, with IC₅₀ values of 16 and 12 μM, respectively^[3].

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

Ronacaleret (SB 751689, 3 mg/kg/day) preserves klotho expression and renal function with the reductions in serum phosphate and albuminuria in 5/6-nephrectomized rats^[3].

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

483.98

C₂₅H₃₂ClF₂NO₄

702686-96-2

O=C(O)CCC1=CC(F)=C(F)C(OC[C@H](O)CNC(C)(C)CC2CC3=C(C=CC=C3)C2)=C1.Cl

Room temperature in continental US; may vary elsewhere.

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

• [1]. György Szabó, et al. Discovery of dihydropyrazino-benzimidazole derivatives as metabotropic glutamate receptor-2 (mGluR2) positive allosteric modulators (PAMs). Eur J Med Chem. 2020 Jan 15:186:111881.  [Content Brief]

  [2]. Tsuneo Takenaka , et al. Antialbuminuric actions of calcilytics in the remnant kidney. Am J Physiol Renal Physiol. 2015 Aug 1;309(3):F216-26.  [Content Brief]

  [3]. Marta Johnson, et al. Inhibition of Intestinal OATP2B1 by the Calcium Receptor Antagonist Ronacaleret Results in a Significant Drug-Drug Interaction by Causing a 2-Fold Decrease in Exposure of Rosuvastatin. Drug Metab Dispos. 2017 Jan;45(1):27-34.  [Content Brief]