2. GPCR/G Protein
  3. CaSR
  4. 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.

Ronacaleret Chemical Structure

Ronacaleret Chemical Structure

CAS No. : 753449-67-1

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Ronacaleret Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
In Vivo

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.

Animal Model: 7-week-old Wistar rats[2].
Dosage: 3 mg/kg/day (dissolved in 10% β-cyclodextrin solution).
Administration: Administered by an osmotic pump that was implanted subcutaneously.
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.
Molecular Weight

447.51

Formula

C25H31F2NO4
CAS No.
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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Purity & Documentation
References
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Ronacaleret Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ronacaleret753449-67-1SB 751689SB751689SB-751689CaSRCalcium-sensing receptorparathyroid hormonepostmenopausal osteoporosisOATP2B1OATP1B1Inhibitorinhibitorinhibit

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