Balicatib

Modify Date: 2024-01-02 16:33:21

Balicatib structure	Common Name	Balicatib
	CAS Number	354813-19-7	Molecular Weight	411.540
	Density	1.2±0.1 g/cm3	Boiling Point	687.4±55.0 °C at 760 mmHg
	Molecular Formula	C₂₃H₃₃N₅O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	369.5±31.5 °C

Use of Balicatib

Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.IC50 value:Target: cathepsin KThe cathepsin K inhibitor AAE-581 (balicatib) as the most advanced of them passed Phase II clinical trials in 2005. Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months (groups O, L, M, H, respectively). Approximately 1 month after treatment initiation, the 50 mg/kg dose was decreased to 30 mg/kg. Twenty animals underwent sham-ovariectomies (group S). Bone mass was measured at 3-6 month intervals. At 18 months, vertebra and femur were collected for histomorphometry.

Name	N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
Synonym	More Synonyms

Description	Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.IC50 value:Target: cathepsin KThe cathepsin K inhibitor AAE-581 (balicatib) as the most advanced of them passed Phase II clinical trials in 2005. Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months (groups O, L, M, H, respectively). Approximately 1 month after treatment initiation, the 50 mg/kg dose was decreased to 30 mg/kg. Twenty animals underwent sham-ovariectomies (group S). Bone mass was measured at 3-6 month intervals. At 18 months, vertebra and femur were collected for histomorphometry.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> Cathepsin Research Areas >> Inflammation/Immunology
References	[1]. Falgueyret JP, et al. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43. [2]. Vasiljeva O, et al. Emerging roles of cysteine cathepsins in disease and their potential as drug targets. Curr Pharm Des. 2007;13(4):387-403. [3]. Jerome C, et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2011 Dec;22(12):3001-11.

Description

Related Catalog

Signaling Pathways >> Metabolic Enzyme/Protease >> Cathepsin

Research Areas >> Inflammation/Immunology

References

[1]. Falgueyret JP, et al. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43.

[2]. Vasiljeva O, et al. Emerging roles of cysteine cathepsins in disease and their potential as drug targets. Curr Pharm Des. 2007;13(4):387-403.

[3]. Jerome C, et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2011 Dec;22(12):3001-11.

Density	1.2±0.1 g/cm3
Boiling Point	687.4±55.0 °C at 760 mmHg
Molecular Formula	C₂₃H₃₃N₅O₂
Molecular Weight	411.540
Flash Point	369.5±31.5 °C
Exact Mass	411.263428
PSA	91.96000
LogP	1.56
Appearance of Characters	white solid
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.590
Storage condition	-20℃

HS Code	2933599090

HS Code	2933599090
Summary	2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(4-propylpiperazin-1-yl)benzamide

Balicatib

N-(1-{[(cyanomethyl)amino]carbonyl}cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide

N-(1-(cyanomethylcarbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide

N-[1-(cyanomethyl-carbamoyl)-cyclohexyl]-4-[4-(1-propyl)-piperazin-1-yl]-benzamide

AAE 581

UNII-E00MVC7O57

Benzamide, N-[1-[[(cyanomethyl)amino]carbonyl]cyclohexyl]-4-(4-propyl-1-piperazinyl)-

N-{1-[(Cyanomethyl)carbamoyl]cyclohexyl}-4-(4-propyl-1-piperazinyl)benzamide

DC Chemicals Limited
China
Product Name: Balicatib
Price: $400.0/100mg $800.0/250mg $1600.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Balicatib
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

Zhejiang Hangyu API Co., Ltd
China
Product Name: Balicatib
Price: ￥Inquiry/1kg
Purity: 99.5%
Stocking Period: Inquiry
Contact: Vinnie

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Price: $145/10mM*1mLinDMSO

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Balicatib

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