| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
| ln Vitro |
In hCaR-HEK293 cells, evocalcet (0, 20 and 60 nM) significantly elevated [Ca2+]i, with a median EC50 value of 92.7 nM [2]. Cytochrome P450 (CYP) isoenzyme cardiovascular activity is not significantly inhibited by evocalcet [2].
|
|---|---|
| ln Vivo |
The effects of evocalcet (0.03 or 0.3 mg/kg; epidermis, once) on calcium and serum parathyroid hormone are reported [1]. For five weeks, Evocalcet (0.3 mg/kg; side, once daily) lowers serum parathyroid hormone.
|
| Animal Protocol |
Animal/Disease Models: Male Sprague Dawley chronic kidney disease (SHPT) with adenine-induced secondary hyperparathyroidism (SHPT) CKD) rats [1]
Doses: 0.03 and 0.3 mg/kg Route of Administration: oral administration and calcium levels, increase inorganic phosphorus in serum [1]. ; 0.03 and 0.3 mg/kg, primary Experimental Results: The 0.3 mg/kg dose diminished serum PTH and Ca levels. |
| References |
|
| Additional Infomation |
Evocalcet has been used in trials studying the treatment of Hyperparathyroidism and Secondary Hyperparathyroidism.
Evocalcet is an orally available calcium receptor (CaR) modulator, with potential calcimimetic activity. Upon administration, evocalcet allosterically binds to and inhibits the activity of CaR, thereby suppressing the production of serum parathyroid hormone (PTH) and prevents the PTH-mediated efflux of calcium from bone and normalizes calcium levels. |
| Molecular Formula |
C24H26N2O2
|
|---|---|
| Molecular Weight |
374.48
|
| Exact Mass |
374.199
|
| CAS # |
870964-67-3
|
| PubChem CID |
71242808
|
| Appearance |
White to off-white solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
594.4±50.0 °C at 760 mmHg
|
| Flash Point |
313.3±30.1 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.666
|
| LogP |
4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
28
|
| Complexity |
517
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
C[C@H](C1=CC=CC2=CC=CC=C21)N[C@H]3CCN(C3)C4=CC=C(C=C4)CC(=O)O
|
| InChi Key |
RZNUIYPHQFXBAN-XLIONFOSSA-N
|
| InChi Code |
InChI=1S/C24H26N2O2/c1-17(22-8-4-6-19-5-2-3-7-23(19)22)25-20-13-14-26(16-20)21-11-9-18(10-12-21)15-24(27)28/h2-12,17,20,25H,13-16H2,1H3,(H,27,28)/t17-,20+/m1/s1
|
| Chemical Name |
2-[4-[(3S)-3-[[(1R)-1-naphthalen-1-ylethyl]amino]pyrrolidin-1-yl]phenyl]acetic acid
|
| Synonyms |
MT4580; MT 4580; MT-4580
|
| 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) |
DMSO : ~30 mg/mL (~80.11 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6704 mL | 13.3518 mL | 26.7037 mL | |
| 5 mM | 0.5341 mL | 2.6704 mL | 5.3407 mL | |
| 10 mM | 0.2670 mL | 1.3352 mL | 2.6704 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
