Product Details
Product Name:
MK-0822 |
CAS No.:
603139-19-1 |
Min. Order:
1G |
Purity:
98% |
Supply Ability:
100KG |
Release date:
2019/07/06 |
AD68
MK-0822 Basic information |
Bioactivity In vitro In vivo Features |
Product Name: |
MK-0822 |
Synonyms: |
Odanacatib,MK-0822,MK0822;Pentanamide, N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]-, (2S)-;(2S)-N-(1-Cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]pentanamide Odanacatib (MK-0822);Odanacatib (2S)-N-(1-Cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]pentanamide;(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide;Odanacatib, >=98%;MK-0822;ODANACATIB |
CAS: |
603139-19-1 |
MF: |
C25H27F4N3O3S |
MW: |
525.564 |
EINECS: |
1533716-785-6 |
Product Categories: |
API;Inhibitors |
Mol File: |
603139-19-1.mol |
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MK-0822 Chemical Properties |
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MK-0822 Usage And Synthesis |
Bioactivity |
Odanacatib (MK-0822) is an effective and selective neutral inhibitor for cathepsin K(human /rabbit) and IC50 is 0.2 nM/1 nM. It has high selectivity for off-target cathepsin B, L, S. Phase 3。 |
In vitro |
In vitro, Odanacatib acts on cathepsin K with high inhibitory activity and selectivity with IC50 of 0.2 nM and 1 nM when it acts on cathepsin K of human and rabbits. Odanacatib is also effective in all human enzyme experiments with IC50 of 5 nM. |
In vivo |
With a dosage of 10 mg/kg acting on preclinical rats, Odanacatib has good pharmacokinetic characteristics such as scavenging activity(Cl: 2 mL kg-1 min-1), low distribution (Vdss: 1.1 L kg-1), half-life(T1/2: 6 h) and Orally bioavailable (F: 8%).In addition, Odanacatib has a good metabolic stability if it acts on the Parental rats with 96% recovery of live. With the dosage of 9 µM, Odanacatib can significantly Increase the Proximal femur bone mineral density (BMD) (7.8%), femoral neck BMD (10.8%) and thighs greater trochanter BMD (6.5%). Long-term treatment with Odanacatib on skeletal matured macaque which is lack of estrogen can efficiently inhibit the bone metabolism, and will not reduce the number of osteoclast. It can also maintain the biomechanics properties of nonhuman primates with Ovary resection (OVX). |
Features |
Odanacatibis an effective and selective neutral inhibitor for cathepsin K |
Company Profile Introduction
Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals.
Mainly deals in the sales of:
Pharmaceutical intermediates
OLED intermediates:
Pharmaceutical intermediates;
OLED intermediates;
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