Ronacaleret hydrochloride
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.
For research use only. We do not sell to patients.
- CAS No.: 702686-96-2
- Formula: C25H32ClF2NO4
- Molecular Weight:483.98
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
Chemical Information
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CAS No. 702686-96-2
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Appearance Solid
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Molecular Weight 483.98
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Formula C25H32ClF2NO4
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Color White to off-white
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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.Cl
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Synonyms
SB 751689A
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Purity & Documentation
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Data Sheet (269 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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)
Ronacaleret hydrochloride Related Classifications
HY-15104 Related Classifications
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