Ronacaleret
Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret (SB 751689) is used for the study of postmenopausal osteoporosis.
For research use only. We do not sell to patients.
- CAS No.: 753449-67-1
- Formula: C25H31F2NO4
- Molecular Weight:447.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
146 nM
Compound: Ronacaleret
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Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
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[PMID: 19442519] |
| HEK293 | IC50 |
320 nM
Compound: Ronacaleret
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Negative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cells
Negative allosteric modulator activity at rat calcium sensing receptor expressed in HEK cells
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[PMID: 19442519] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:7-week-old Wistar rats[2].
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Dosage:3 mg/kg/day (dissolved in 10% β-cyclodextrin solution).
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Administration:Administered by an osmotic pump that was implanted subcutaneously.
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Result:Increased renal expression of klotho in a dose-dependent manner.
Decreased serum phosphate and FGF23 with the increased fractional excretion of phosphate without changes in serum calcium.
Appeared to similarly protect podocytes.
Reduced FGF23 and because FGF23 enhanced klotho expression.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 753449-67-1
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Molecular Weight 447.51
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Formula C25H31F2NO4
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SMILES
O=C(O)CCC1=CC(F)=C(F)C(OC[C@H](O)CNC(C)(C)CC2CC3=C(C=CC=C3)C2)=C1
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Synonyms
SB 751689
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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