1. GPCR/G Protein
  2. CaSR
  3. Ronacaleret hydrochloride

Ronacaleret hydrochloride  (Synonyms: SB 751689A)

Cat. No.: HY-15104
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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.

Ronacaleret hydrochloride Chemical Structure

Ronacaleret hydrochloride Chemical Structure

CAS No. : 702686-96-2

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Based on 1 publication(s) in Google Scholar

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Description

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].

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.

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

483.98

Formula

C25H32ClF2NO4

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

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
References
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Ronacaleret hydrochloride Related Classifications

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Help & FAQs
  • 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.

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Ronacaleret hydrochloride
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HY-15104
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