| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Ronacaleret inhibits the in vitro activities of OATP1B1 (IC50 = 11 μM) and OATP2B1 (IC50 = 12 μM) without inhibiting BCRP[3]. Ronacaleret was shown to inhibit the uptake of the probe substrate estradiol-glucuronide mediated by OATP1B1 and OATP1B3 with relatively low potency (IC50 values of 11 and 60 μM, respectively)[3]. Ronacaleret inhibits OATP2B1-mediated transport of rosuvastatin at pH 7.4 and pH 6.0 with IC50 values of 16 and 12 μM, respectively[3].
|
|---|---|
| ln Vivo |
Ronacaleret (SB 751689, 3 mg/kg/day) preserved klotho expression and renal function while reducing serum phosphorus and albuminuria in 5/6 nephrectomized rats[3].
|
| Animal Protocol |
Animal/Disease Models: 7-week-old Wistar rats[2].
Doses: 3 mg/kg/day (dissolved in 10% β-cyclodextrin solution). Route of Administration: Administered by an osmotic pump that was implanted subcutaneously. Experimental Results: 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. |
| References |
|
| Additional Infomation |
Ronacaleret is a calcium-sensing receptor antagonist.
Drug Indication Post-menopausal women with osteoporosis Mechanism of Action 751689 is novel small molecules that work by antagonizing calcium-sensing receptors on the surface of the parathyroid gland, thereby triggering a transient release of the body's own stores of parathyroid hormone (PTH). This release of PTH may have the potential to rebuild the bone mass lost as a result of osteoporosis and improve overall bone microarchitecture in these patients. |
| Molecular Formula |
C25H31F2NO4
|
|---|---|
| Molecular Weight |
447.51
|
| Exact Mass |
449.238
|
| CAS # |
753449-67-1
|
| PubChem CID |
10345214
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
4.749
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
32
|
| Complexity |
591
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(C)(CC1CC2=CC=CC=C2C1)NC[C@H](COC3=C(C(=CC(=C3)CCC(=O)O)F)F)O
|
| InChi Key |
FQJISUPNMFRIFZ-HXUWFJFHSA-N
|
| InChi Code |
InChI=1S/C25H31F2NO4/c1-25(2,13-17-9-18-5-3-4-6-19(18)10-17)28-14-20(29)15-32-22-12-16(7-8-23(30)31)11-21(26)24(22)27/h3-6,11-12,17,20,28-29H,7-10,13-15H2,1-2H3,(H,30,31)/t20-/m1/s1
|
| Chemical Name |
3-[3-[(2R)-3-[[1-(2,3-dihydro-1H-inden-2-yl)-2-methylpropan-2-yl]amino]-2-hydroxypropoxy]-4,5-difluorophenyl]propanoic acid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2346 mL | 11.1729 mL | 22.3459 mL | |
| 5 mM | 0.4469 mL | 2.2346 mL | 4.4692 mL | |
| 10 mM | 0.2235 mL | 1.1173 mL | 2.2346 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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