Relacatib
Based on 1 Customer Validation
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.
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- Pureté : 99.58%
- CAS No.: 362505-84-8
- Formule: C27H32N4O6S
- Masse moléculaire:540.63
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Stockage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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cathepsin K |
cathepsin L |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
14 nM
Compound: relacatib
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Inhibition of cathepsin B in human HepG2 cells
Inhibition of cathepsin B in human HepG2 cells
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[PMID: 18226527] |
| HepG2 | IC50 |
2 nM
Compound: relacatib
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Inhibition of cathepsin L in human HepG2 cells
Inhibition of cathepsin L in human HepG2 cells
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[PMID: 18226527] |
| Osteoclast | IC50 |
15 nM
Compound: relacatib
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Inhibition of bone resorption in rabbit osteoclast
Inhibition of bone resorption in rabbit osteoclast
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[PMID: 18226527] |
| Osteoclast | IC50 |
20 nM
Compound: 10
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Effect on collagen accumulation in osteoclast bone resorption assay
Effect on collagen accumulation in osteoclast bone resorption assay
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[PMID: 16509577] |
| Ramos | IC50 |
8 nM
Compound: relacatib
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Inhibition of cathepsin S in human ramos cells
Inhibition of cathepsin S in human ramos cells
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[PMID: 18226527] |
In Vitro
Relacatib are incubated with human osteoclastoma-derived osteoclasts seeded onto bovine cortical bone slices in vitro biological activity, it shows inhibitory potency with Ki values of 0.041 nM, 0.068 nM,0.063 nM,1.6 nM,and 13 nM against human cathepsin K, cathepsin L, cathepsin V, cathepsin S and cathepsin B, respectively in the assay[1]. Relacatib is against Monkey cathepsin K, cathepsin L,cathepsin V and cathepsin B with Ki values of 0.041 nM, 0.28 nM, 0.72 nM and 11nM, respectively. Relacatib is against mouse cathepsin L and rat cathepsin L with Ki values of 0.20 nM and 0.17 nM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus monkey[2]
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Dosage:12 mg/kg
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Administration:Subcutaneous injection; single dose; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration
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Result:Was sufficiently high to significantly suppress bone resorption from 1.5 to 72 h post dosing.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 362505-84-8
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Appearance Solid
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Masse moléculaire 540.63
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Formule C27H32N4O6S
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Color White to off-white
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SMILES
O=C(C1=CC2=CC=CC=C2O1)N[C@H](C(N[C@@H]3C(CN(S(=O)(C4=NC=CC=C4)=O)[C@H](C)CC3)=O)=O)CC(C)C
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Synonyms
SB-462795
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvant et solubilité
In Vitro:
DMSO : 40 mg/mL (73.99 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Protocole
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Osteoclast differentiation from monocyte/macrophage precursors
Osteoclast differentiation is an in vitro induction assay in which monocyte/macrophage-lineage precursors are exposed to macrophage colony-stimulating factor (M-CSF) and receptor activator of NF-κB ligand (RANKL), generating multinucleated osteoclasts that are commonly identified by tartrate-resistant acid phosphatase (TRAP) staining and functionally confirmed by resorption pits on dentin, bone, or mineralized substrates. M-CSF supports survival and expansion of osteoclast precursors, while RANKL binding to RANK drives osteoclast commitment, fusion, maturation, and resorptive function; osteoprotegerin inhibits this pathway by binding RANKL and preventing RANK activation. The main readouts are the number of TRAP-positive multinucleated cells, formation of F-actin rings, and resorbed surface area; TRAP-positive multinucleated cells indicate osteoclast differentiation, whereas pit formation on dentin, bone, or mineralized coating indicates functional bone-resorbing activity.
Pureté et documentation
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Fiche technique (274 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Dennis S Yamashita, et al. Structure Activity Relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one Cathepsin K Inhibitors.J Med Chem [Content Brief]
[2]. S Kumar, et al.A Highly Potent Inhibitor of Cathepsin K (Relacatib) Reduces Biomarkers of Bone Resorption Both in Vitro and in an Acute Model of Elevated Bone Turnover in Vivo in Monkeys.Bone. 2007 Jan;40(1):122-31. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8497 mL | 9.2485 mL | 18.4969 mL | 46.2423 mL |
| 5 mM | 0.3699 mL | 1.8497 mL | 3.6994 mL | 9.2485 mL | |
| 10 mM | 0.1850 mL | 0.9248 mL | 1.8497 mL | 4.6242 mL | |
| 15 mM | 0.1233 mL | 0.6166 mL | 1.2331 mL | 3.0828 mL | |
| 20 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3121 mL | |
| 25 mM | 0.0740 mL | 0.3699 mL | 0.7399 mL | 1.8497 mL | |
| 30 mM | 0.0617 mL | 0.3083 mL | 0.6166 mL | 1.5414 mL | |
| 40 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1561 mL | |
| 50 mM | 0.0370 mL | 0.1850 mL | 0.3699 mL | 0.9248 mL | |
| 60 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL |
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