Art. -Nr.: HY-10294

Relacatib

Name: Relacatib
Brand: MedChemExpress
SKU: HY-10294
Price: 523.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: SB-462795)

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Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with K_i 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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Reinheit : 99.58%
CAS. Nr.: 362505-84-8
Formel: C₂₇H₃₂N₄O₆S
Molecular Weight:540.63

Speicherung:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Relacatib Chemical Structure

CAS. Nr.: 362505-84-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (2)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

cathepsin K

cathepsin L

Alle Cathepsin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	14 nM Compound: relacatib	Inhibition of cathepsin B in human HepG2 cells Inhibition of cathepsin B in human HepG2 cells	[PMID: 18226527]
HepG2	IC₅₀	2 nM Compound: relacatib	Inhibition of cathepsin L in human HepG2 cells Inhibition of cathepsin L in human HepG2 cells	[PMID: 18226527]
Osteoclast	IC₅₀	15 nM Compound: relacatib	Inhibition of bone resorption in rabbit osteoclast Inhibition of bone resorption in rabbit osteoclast	[PMID: 18226527]
Osteoclast	IC₅₀	20 nM Compound: 10	Effect on collagen accumulation in osteoclast bone resorption assay Effect on collagen accumulation in osteoclast bone resorption assay	[PMID: 16509577]
Ramos	IC₅₀	8 nM Compound: relacatib	Inhibition of cathepsin S in human ramos cells Inhibition of cathepsin S in human ramos cells	[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 K_i 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 K_i 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 K_i 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

Relacatib (1-2 mg/kg 0.5 h intravenous infusion; 2-4 mg/kg oral bolus gavage) exhibits T_1/2, CL or V_dss with 109 mins, 19.5 mL/min/kg, or 1.86 L/kg in male Sprague-Dawley rats and 168 mins, 11.7 mL/min/kg, and 1.79 L/kg in monkeys, respectively in a PK iv/po crossover studies. The oral bioavailability of Relacatib is 28% in the monkey and 89.4% in the rats^[1].
SB-462795 (subcutaneous injection; 12 mg/kg; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration) significantly inhibits resorption as assessed by two markers of bone resorption,the N- (NTx) and C-telopeptides (CTx) of type I collagen measured in serum. SB-462795 does not exhibit difference of serum osteocalcin (a biomarker of osteoblast activity) between SB-462795 and vehicle treated animalsexcept for the 48 h time point where a significant reduction (42% lower than baseline vs. 18% lower than baseline with vehicle treatment)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Cynomolgus monkey^[2]
Dosage:

12 mg/kg
Administration:

Subcutaneous injection; single dose; blood sample is drawn 1.5, 4, 24, 48, and 72 h post dose administration
Result:

Was sufficiently high to significantly suppress bone resorption from 1.5 to 72 h post dosing.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 362505-84-8
Appearance Solid
Molecular Weight 540.63
Formel C₂₇H₃₂N₄O₆S
Color White to off-white
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
Synonyms

SB-462795
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8497 mL

9.2485 mL

18.4969 mL

5 mM

0.3699 mL

1.8497 mL

3.6994 mL

10 mM

0.1850 mL

0.9248 mL

1.8497 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

SB-462795 (12 mg/kg) or vehicle is in 70% aqueous PEG400(1 ml/kg)^[2].

Protocol 2

SSB-462795 is prepared as a nanosuspension containing 1.5% Methylcellulose and 2.0% sodium lauryl sulfate^[2].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Relacatib

Alle Cathepsin Isoform-spezifische Produkte anzeigen